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Journal articles on the topic 'Indole moiety'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Li, Jiao, and Chun-Lin Zhuang. "Natural Indole Alkaloids from Marine Fungi: Chemical Diversity and Biological Activities." Pharmaceutical Fronts 03, no. 04 (2021): e139-e163. http://dx.doi.org/10.1055/s-0041-1740050.

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The indole scaffold is one of the most important heterocyclic ring systems for pharmaceutical development, and serves as an active moiety in several clinical drugs. Fungi derived from marine origin are more liable to produce novel indole-containing natural products due to their extreme living environments. The indole alkaloids from marine fungi have drawn considerable attention for their unique chemical structures and significant biological activities. This review attempts to provide a summary of the structural diversity of marine fungal indole alkaloids including prenylated indoles, diketopip

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2

Gaikwad, Vijay. "Review of indole, A versatile pharmacophoric moiety." Current Trends in Pharmacy and Pharmaceutical Chemistry 6, no. 2 (2024): 34–40. http://dx.doi.org/10.18231/j.ctppc.2024.011.

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Indole is a heterocyclic compound, known for its alluring smell. Indole contributes to the rich aroma of various flowers such as jasmine and orange blossoms. Indole plays a vital role in numerous biological processes, including hormone regulation, neurotransmission, and immune response. Indole derivatives serve as a foundation for developing drugs in several therapeutic areas, such as antiviral, anticancer, and psychiatric medications.

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3

Padrtová, Tereza, Pavlína Marvanová, Renáta Kubínová, et al. "Indol-2-Carboxylic Acid Esters Containing N-Phenylpiperazine Moiety - Preparation and Cholinesterase-inhibiting Activity." Current Organic Synthesis 17, no. 7 (2020): 576–87. http://dx.doi.org/10.2174/1570179417666200619132218.

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Background: The indole derivatives and the N-phenylpiperazine fragment represent interesting molecular moieties suitable for the research of new potentially biologically active compounds. This study was undertaken to identify if indol-2-carboxylic acid esters containing N-phenylpiperazine moiety possess acetylcholinesterase and butyrylcholinesterase inhibitory activity. Materials and Methods: The study dealt with the synthesis of a novel series of analogs of 1H-indole-2- carboxylic acid and 3-methyl-1H-indole-2-carboxylic acid. The structure of the derivatives was represented by the indolylcar

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4

Qin, Wenling, Nan Zhang, Yige Li, and Zhili Chen. "Direct Preparation of Indole Hemiaminals through Organocatalytic Nucleophilic Addition of Indole to Aldehydes." Synthesis 50, no. 20 (2018): 4063–70. http://dx.doi.org/10.1055/s-0037-1610453.

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Hemiaminals are common in natural products as well as bioactive compounds. Hemiaminals with an indole moiety are particularly attractive due to the significant bioactivity of indoles. Herein, we reported an efficient organocatalyzed indole N-1 nucleophilic addition of α-oxoaldehydes to deliver various indole hemiaminals in good yields (up to 92%) and excellent regioselectivities with DABCO or triethylamine as the catalyst. The method is characterized by mild reaction conditions, widely available reagents, and general substrate scope, and it is also applicable to late-stage transformations with

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5

Hájíček, Josef. "A Review on Recent Developments in Syntheses of the post-Secodine Indole Alkaloids. Part II: Modified Alkaloid Types." Collection of Czechoslovak Chemical Communications 72, no. 7 (2007): 821–98. http://dx.doi.org/10.1135/cccc20070821.

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The second part of the planned review on developments in the field of total and formal total synthesis of the post-secodine indole alkaloids concentrates on modified alkaloid types, i.e. those skeletons derived from primary types by formation of additional and/or rupture of existing bonds, while connectivities next to indol(e)ine moiety remain intact. It thus reviews the synthesis of alkaloids of quebrachamine/cleavamine type including VLB-bis-indoles, rhazinilam type, aspidofractinine/kopsane and kopsifoline type, as well as kopsijasminilam alkaloids, lapidilectine B and danuphylline. It cove

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6

Naraboli, Basavaraj Shivabasappa, and Jayaprakash Sharanappa Biradar. "SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF INDOLE DERIVATIVES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE MOIETY." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 8 (2017): 128. http://dx.doi.org/10.22159/ijpps.2017v9i8.19725.

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Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives viz., 2-((1H-benzo[d]imidazol-2-yl)thio)-N-(4-(3-(1H-indol-3-yl)acryloyl)phenyl)acetamide 6a-d, N-(4-(3-(1H-indol-3-yl)acryloyl)phenyl)-2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio)acetamide 7a-d and N-(4-(3-(1H-indol-3-yl)acryloyl)phenyl)-2-(benzo[d]thiazol-2-ylthio)acetamide 8a-d.Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities: like 1,1-diphenyl-2-picryl hydrazyl

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7

Gardette, Daniel, Jean-Claude Gramain, Marie-Eve Lepage, and Yves Troin. "Photocyclization of aryl enaminones. An efficient route to indole alkaloid synthons." Canadian Journal of Chemistry 67, no. 2 (1989): 213–19. http://dx.doi.org/10.1139/v89-036.

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The photocyclization of enaminones was extended to aryl enaminones bearing a substituent on the aromatic moiety. This reaction was studied in order to achieve the synthesis of indole alkaloid synthons. Trials of regioselectivity control were made by using groups with enhanced steric hindrance. The reactivity of secondary enaminones was tested, and the ratio of C-alkylation to N-alkylation was shown to be dependent on the nature of the aromatic substituent. During this work, new hexahydrocarbazolones were synthesized, with substituents on the A ring or the modified C ring. Keywords: photocycliz

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8

Selvanayagam, S., B. Sridhar, S. Kathiravan, and R. Raghunathan. "Methyl (2Z)-2-[(2-formyl-3-methyl-1H-indol-1-yl)methyl]-3-(4-methoxyphenyl)prop-2-enoate." Acta Crystallographica Section E Structure Reports Online 70, no. 4 (2014): o431—o432. http://dx.doi.org/10.1107/s1600536814005261.

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In the title indole derivative, C22H21NO4, the dihedral angle between the benzene and pyrrole rings of indole moiety is 1.8 (1)°. The plane of the 4-methoxyphenyl ring is oriented with a dihedral angle of 60.7 (1)° with respect to the plane of the indole moiety. The molecular packing is stabilized by C—H...O hydrogen bonds which form a V-shaped chain arrangement along thebcplane of the unit cell. In addition to this, C—H...π and π–π interactions [centroid–centroid distances = 3.8102 (11) and 3.8803(12) Å], which run along theb-axis direction, stabilize the molecular packing.

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9

Zhang, Dongdong, Yanhong Shi, Jingyi Li, et al. "Alkaloids with Nitric Oxide Inhibitory Activities from the Roots of Isatis tinctoria." Molecules 24, no. 22 (2019): 4033. http://dx.doi.org/10.3390/molecules24224033.

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As our ongoing research project on Ban Lan Gen (Isatis tinctoria roots), a total of 23 alkaloids were obtained. Compounds 1 and 2 contain an unusual C–C bond between the 2(1H)-quinolinone moiety and the phenol moiety and between the 2(1H)-quinolinone moiety and the 1H-indole moiety, respectively. Compound 3 possesses an unusual carbon skeleton and its putative biosynthetic pathway was discussed, and Compound 23 was deduced as a new indole alkaloid glycoside. Compounds 4–7 were identified as four new natural products by extensive spectroscopic experiments. Additionally, the anti-inflammatory ac

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10

Kochetkov, Konstantin A., Olga N. Gorunova, and Natalia A. Bystrova. "Biologically Oriented Hybrids of Indole and Hydantoin Derivatives." Molecules 28, no. 2 (2023): 602. http://dx.doi.org/10.3390/molecules28020602.

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Indoles and hydantoins are important heterocycles scaffolds which present in numerous bioactive compounds which possess various biological activities. Moreover, they are essential building blocks in organic synthesis, particularly for the preparation of important hybrid molecules. The series of hybrid compounds containing indoles and imidazolidin-2-one moiety with direct C–C bond were synthesized using an amidoalkylation one-pot reaction. All compounds were investigated as a growth regulator for germination, growth and development of wheat seeds (Triticum aestivum L). Their effect on drought r

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11

Si, Ying-Ying, Wei-Wei Wang, Qing-Mei Feng, et al. "Neuroinflammatory inhibitors from Gardneria nutans Siebold & Zuccarini." RSC Advances 11, no. 44 (2021): 27085–91. http://dx.doi.org/10.1039/d1ra05204g.

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Four new compounds were isolated from G. nutans. Compounds 1–2 are two rare monoterpene indole alkaloids with the glucosyl moiety located at C-12 and represent the first two examples of enantiomer of ajmaline type monoterpene indole alkaloids.

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12

Dinda, Enakshi, Samir Kumar Bhunia та Ranjan Jana. "Palladium-Catalyzed Cascade Reactions for Annulative π -Extension of Indoles to Carbazoles through C–H Bond Activation". Current Organic Chemistry 24, № 22 (2020): 2612–33. http://dx.doi.org/10.2174/1385272824999200817170058.

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The annulative &#960;-extension (APEX) reactions through C-H bond activation has tremendous potential to access fused aromatic systems from relatively simple aromatic compounds in a single step. This state-of-the-art technique has the ability to streamline the synthesis of functionalized materials useful in material science, biomedical research, agroand pharmaceutical industries. Furthermore, C-H activation strategy does not require prefunctionalization steps, which allows for the late-stage modification of the functional molecule with requisite molecular properties. Owing to their unique

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13

Marianna, Budovska, Michalkova Radka, Kello Martin, Vaskova Janka, and Mojzis Jan. "Design, Synthesis and Antiproliferative Evaluation of Bis-Indole Derivatives with a Phenyl Linker: Focus on Autophagy." Molecules 28, no. 1 (2022): 251. http://dx.doi.org/10.3390/molecules28010251.

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This work deals with the study of the synthesis of new bis-indole analogues with a phenyl linker derived from indole phytoalexins. Synthesis of target bis-indole thiourea linked by a phenyl linker was achieved by the reaction of [1-(tert-butoxycarbonyl)indol-3-yl]methyl isothiocyanate with p-phenylenediamine. By replacing the sulfur of the thiocarbonyl group in bis-indole thiourea with oxygen using mesityl nitrile oxide, a bis-indole homodimer with a urea group was obtained. A cyclization protocol utilizing bis-indole thiourea and methyl bromoacetate was applied to synthesize a bis-indole homo

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14

Kitajima, Mariko, Tetsuya Koyama, Yuqiu Wu, Noriyuki Kogure, Rongping Zhang, and Hiromitsu Takayama. "Kopsiyunnanines J1 and J2, New Strychnos-type Homo-Monoterpenoid Indole Alkaloids from Kopsia arborea." Natural Product Communications 10, no. 1 (2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000114.

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Two new indole alkaloids, kopsiyunnanines J1 and J2, were isolated from Yunnan Kopsia arborea, and their structures were determined by spectroscopic analyses. Kopsiyunnanines J1 and J2 are unprecedented Strychnos-type indole alkaloids having an additional C1 unit in the secologanin moiety of the molecule.

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15

Iwatsuki, Satoshi, Takuya Suzuki, Syogo Tanooka, Tatsuo Yajima, and Yuichi Shimazaki. "Kinetic studies on cyclopalladation in palladium(II) complexes containing an indole moiety." Pure and Applied Chemistry 86, no. 2 (2014): 151–61. http://dx.doi.org/10.1515/pac-2014-5020.

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Abstract Various Pd–C complexes have been developed to date, affording deep insights into the reaction intermediates in useful catalytic reactions in organic syntheses. Cyclopalladation is one of the most famous Pd–C bond formation reactions to generate the palladacycles. Indole is an electron-rich aromatic ring involved in the side chain of an essential amino acid, tryptophan (Trp), and Trp and its derivatives are important in biological systems, such as electron transfer in protein, cofactors for conversion of biological molecules and so on. Pd catalysts are also useful for syntheses of such

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16

Mir, Reyaz Hassan, Roohi Mohi-ud-din, Taha Umair Wani, et al. "Indole: A Privileged Heterocyclic Moiety in the Management of Cancer." Current Organic Chemistry 25, no. 6 (2021): 724–36. http://dx.doi.org/10.2174/1385272825666210208142108.

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Heterocyclic are a class of compounds that are intricately entwined into life processes. Almost more than 90% of marketed drugs carry heterocycles. Synthetic chemistry, in turn, allocates a cornucopia of heterocycles. Among the heterocycles, indole, a bicyclic structure consisting of a six-membered benzene ring fused to a five-membered pyrrole ring with numerous pharmacophores that generate a library of various lead molecules. Due to its profound pharmacological profile, indole got wider attention around the globe to explore it fully in the interest of mankind. The current review covers recent

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17

Cui, Hai-Lei, Yin Shi, Hui-Qing Deng та ін. "Catalyst-Free Synthesis of Aminals from Indole-Derived α,α-Dicyanoolefins". Synlett 30, № 02 (2018): 167–72. http://dx.doi.org/10.1055/s-0037-1611940.

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We have developed an efficient synthesis of indole fused aminals with nucleophilic imines and indole-derived α,α-dicyanoolefins via N-sulfonyl group transfer. The combination of two privileged frameworks, tetrahydroisoquinoline or tetrahydro-β-carboline and indole, can be realized by this approach to the construction of aminals. The synthetic application of this method was further demonstrated by the straightforward transformations into highly functionalized aminals possessing carbonyl groups through oxidative cleavage of the nitrile moiety.

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18

Allart-Simon, Ingrid, Aurélie Moniot, Nicolo Bisi, et al. "Pyridazinone derivatives as potential anti-inflammatory agents: synthesis and biological evaluation as PDE4 inhibitors." RSC Medicinal Chemistry 12, no. 4 (2021): 584–92. http://dx.doi.org/10.1039/d0md00423e.

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19

Rekiba, Nawel, Abdelmadjid Benmohammed, Sofiane Khanoussi, Ayada Djafri, and Jérôme Thibonnet. "Synthesis and Characterization of Novel Thiazolidinones and Thioxothiazolidinones Derived from Substituted Indole." Molbank 2021, no. 4 (2021): M1284. http://dx.doi.org/10.3390/m1284.

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Based on recent discoveries concerning the numerous biological properties of thiazolidinones and thiosemicarbazones, new N-substituted heterocyclic derivatives have been designed by combining the indole ring with thioxothiazolidinone, thiazolidinone or thiosemicarbazone. Thus, a series of new thioxothiazolidinone, thiazolidinone, or thiosemicarbazone derivatives bearing indole-based moiety have been designed, synthesized, and developed in good yields.

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20

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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21

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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22

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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23

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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24

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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25

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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26

Bębenek, Ewa, Elwira Chrobak, Zuzanna Rzepka, and Dorota Wrześniok. "New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro." Biomolecules 12, no. 10 (2022): 1540. http://dx.doi.org/10.3390/biom12101540.

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As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of the ester derivatives obtained in the Steglich reaction was confirmed by spectroscopic methods (1H and 13C NMR, HR-MS). The obtained new 3-indolyl betulin derivatives were evaluated for anticancer activity against several human cancer cell lines (melanomas, breast cancers, colorectal adenocarcinomas, lung cancer) as well as normal human fibroblasts. The significant reduction in MCF-7 cell

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27

Mahapatra, Ajit Kumar, Kalipada Maiti, Rajkishor Maji, et al. "Ratiometric fluorescent and chromogenic chemodosimeter for cyanide detection in water and its application in bioimaging." RSC Advances 5, no. 31 (2015): 24274–80. http://dx.doi.org/10.1039/c4ra17199c.

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28

Sarasiya, Shahir, Sara Sarasiya, and Maged Henary. "Exploration of NIR Squaraine Contrast Agents Containing Various Heterocycles: Synthesis, Optical Properties and Applications." Pharmaceuticals 16, no. 9 (2023): 1299. http://dx.doi.org/10.3390/ph16091299.

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Squaraine dye is a popular class of contrast near-infrared (NIR) dyes. Squaraine dyes have shown the ability to be modified with various heterocycles. The indole moiety is the most notable heterocycle incorporated in squaraine dyes. A tremendous amount of work has gone into developing indole-based squaraine dyes and determining their applications. The optical properties of squaraine dyes containing an indole moiety facilitate high quantum yields and molar absorptivity, but the absorbance maxima is capped near 700 nm. This is the major limitation of indole-based squaraine dyes. In comparison, o

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29

Munir, Samman, Aqsa Shahid, Bilal Aslam, et al. "The Therapeutic Prospects of Naturally Occurring and Synthetic Indole Alkaloids for Depression and Anxiety Disorders." Evidence-Based Complementary and Alternative Medicine 2020 (October 16, 2020): 1–11. http://dx.doi.org/10.1155/2020/8836983.

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Depression and anxiety are the most common disorders among all age groups. Several antidepressant drugs including benzodiazepine, antidepressant tricyclics, azapirone, noradrenaline reuptake inhibitors, serotonin selective reuptake inhibitors, serotonin, noradrenaline reuptake inhibitors, and monoamine oxidase inhibitors have been used to treat these psychiatric disorders. However, these antidepressants are generally synthetic agents and can cause a wide range of side effects. The potential efficacy of plant-derived alkaloids has been reviewed against various neurodegenerative diseases includi

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Leifert, Dirk, Denis G. Artiukhin, Johannes Neugebauer, Anzhela Galstyan, Cristian Alejandro Strassert, and Armido Studer. "Radical perfluoroalkylation – easy access to 2-perfluoroalkylindol-3-imines via electron catalysis." Chemical Communications 52, no. 35 (2016): 5997–6000. http://dx.doi.org/10.1039/c6cc02284g.

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Enomoto, Masaru. "Recent advances in the total syntheses of indole diterpenoids." Bioscience, Biotechnology, and Biochemistry 85, no. 1 (2021): 13–23. http://dx.doi.org/10.1093/bbb/zbaa061.

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Abstract Indole diterpenoids constitute a large family of natural products that are characterized by a hybrid molecular architecture consisting of an indole nucleus and diterpenoid moiety. Their pharmacologically and agriculturally important biological properties as well as intriguing molecular architectures have attracted much attention from many synthetic organic chemists. In 2012, we succeeded in the concise total synthesis of a paspalane-type indole diterpenoid, namely paspalinine, by developing a highly efficient indole ring formation protocol. After the report of this total synthesis, 4

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Hájíček, Josef. "Recent developments in syntheses of the post-secodine indole alkaloids. Part III: Rearranged alkaloid types." Collection of Czechoslovak Chemical Communications 76, no. 12 (2011): 2023–83. http://dx.doi.org/10.1135/cccc2011099.

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The third part of a planned review on developments in the field of total and formal total synthesis of the post-secodine indole alkaloids focuses on types of rearranged alkaloids, i.e. on the skeletons with altered connectivities next to the indol(e)ine moiety, especially with a new bond to N-1. It reviews the synthesis of melodane, goniomitine, chippiine/dippinine, lirofoline and tronocarpine alkaloids, as well as alkaloids of secoschizozygane/vallesamidine, schizozygane and isoschizozygane type. It covers the literature from approximately 1991 up to May 2011. A review with 115 references.

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L., Krishnakumar K., Mathew Paul Ukken та Manju R. "A STUDY ON EFFECT OF INDOLE AS A SUBSTITUENT ON A KETO-ENOL TAUTOMER: A SYNTHETIC APPROACH ON β-DIKETONE". International Journal of Pharmacy and Pharmaceutical Sciences 9, № 8 (2017): 219. http://dx.doi.org/10.22159/ijpps.2017v9i8.19576.

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Objective: The existence of keto-enol tautomerism in β-diketones can typically study by a choice of analytical technique. The position of the keto-enol equilibrium depends on a number of factors like solvent, temperature, and substituents. Here an attempt was made to examine the effect of indole, a heterocyclic moiety with the moderately high polar surface area to examine its effect on ketonisation of β-diketone.Methods: The β-diketone studied and synthesized is a structural analog of magical drug curcumin. The structural influence of indole on ketonisation of β-diketone is studied to give a h

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34

Selvanayagam, S., B. Sridhar, S. Kathiravan, and R. Raghunathan. "Crystal structure of methyl (2Z)-3-(4-chlorophenyl)-2-[(3-methyl-1H-indol-1-yl)methyl]prop-2-enoate." Acta Crystallographica Section E Crystallographic Communications 71, no. 6 (2015): 720–22. http://dx.doi.org/10.1107/s2056989015010002.

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In the title indole derivative, C20H18ClNO2, the chlorophenyl ring is almost perpendicular to the indole moiety, making a dihedral angle of 87.6 (1)°. The molecular packing is stabilized by C—H...π interactions, which form aC(9) chain motif along [10-1]. In addition, there are weak π–π interactions [centroid–centroid distance 3.851 (1) Å] between the chains, involving inversion-related chlorophenyl rings.

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Rzepka, Zuzanna, Ewa Bębenek, Elwira Chrobak, and Dorota Wrześniok. "Synthesis and Anticancer Activity of Indole-Functionalized Derivatives of Betulin." Pharmaceutics 14, no. 11 (2022): 2372. http://dx.doi.org/10.3390/pharmaceutics14112372.

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Pentacyclic triterpenes, including betulin, are widespread natural products with various pharmacological effects. These compounds are the starting material for the synthesis of substances with promising anticancer activity. The chemical modification of the betulin scaffold that was carried out as part of the research consisted of introducing the indole moiety at the C-28 position. The synthesized new 28-indole-betulin derivatives were evaluated for anticancer activity against seven human cancer lines (A549, MDA-MB-231, MCF-7, DLD-1, HT-29, A375, and C32). It was observed that MCF-7 breast canc

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Ramesh, Dandagvhal Kamlesh, та Chatpalliwar Vivekanand Arvind. "Synthesis, Characterization and in vitro Studies of Some Ethyl 2-Carboxylate-5- monosubstitued 1H-indole Derivatives as Potential GSK-3β Inhibitors". Asian Journal of Organic & Medicinal Chemistry 7, № 2 (2022): 221–25. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p390.

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The present work focuses on indole derivatives due to their promising inhibition activity toward GSK-3β. New compounds based on the indole moiety were synthesized via Japp-Klingemann indole synthesis. The structures of the new compounds were elucidated on the basis of their FTIR, 1H NMR, 13C NMR spectral data, GC-HRMS and elemental analysis. The in vitro GSK-3β inhibitory activity of the new compounds was evaluated using a luminance assay technique in terms of IC50. Compound Aii11 showed excellent inhibitory activity. Compounds Aii2, Aii1 and Aii3 presented promising GSK-3β inhibitory activity

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Al-Qawasmeh, Raed A., Louy A. Al-Nazer, Sarah A. Dawlat-Kari, et al. "Design, Synthesis and Characterization of Novel Isoxazole Tagged Indole Hybrid Compounds." Open Chemistry 18, no. 1 (2020): 138–48. http://dx.doi.org/10.1515/chem-2020-0017.

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AbstractSixteen new isoxazole tagged indole compounds have been synthesized via copper (I) catalyzed click chemistry of the aryl hydroxamoyl chloride and an indole containing alkyne moiety. The chemical structure of the synthesized compounds has been established using various physicochemical techniques. X-ray single crystal analysis of Ethyl 1-((3-phenylisoxazol-5-yl) methyl)-1H-indole-2-carboxylate (8a) has been analyzed. All compounds were tested for their antibacterial and anticancer activities. The activities for the new compounds were weak against both bacterial strains and the cancer cel

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Wu, Shu-Fang, Man-Su Tu, Qing-Qing Hang, et al. "Construction of chiral chroman scaffolds via catalytic asymmetric (4 + 2) cyclizations of para-quinone methide derivatives with 3-vinylindoles." Organic & Biomolecular Chemistry 18, no. 28 (2020): 5388–99. http://dx.doi.org/10.1039/d0ob01049a.

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The title reaction has been established in the presence of chiral phosphoric acid, affording chiral chroman derivatives bearing an indole moiety in high yields and with moderate to good stereoselectivities.

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Pawar, Kalpana, Anshuman Yadav, Parteek Prasher, et al. "Identification of an indole–triazole–amino acid conjugate as a highly effective antifungal agent." MedChemComm 6, no. 7 (2015): 1352–59. http://dx.doi.org/10.1039/c5md00156k.

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Compounds constructed by the grafting of amino acid and triazole with an indole moiety were synthesized and investigated for antifungal activities wherein one of the compounds gave highly promising results.

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C., Buvana* R. Suresh1 Y. Haribabu P. K. Manna. "INDOLES AS THERAPEUTICS OF INTEREST IN MEDICINAL CHEMISTRY." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 03 (2018): 1585–602. https://doi.org/10.5281/zenodo.1206386.

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Indole is a valuable compound which has becomeprominent in medicinal chemistry because of its variousbiological activities. Indole ring is present in various marineor terrestrial natural compounds, which have useful biologicalproperties. In last few years it was reported that indole, itsbioisosters and derivatives had antimicrobial activity againstgramnegative, grampositive bacteria and yeast candidaalbicans antimicrobial activity. A large number of efforts were made to synthesizedifferent heterocyclic compounds and their derivatives in thepast decode and were found to possess promising antitu

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Phan, Thi Ha My, Yu-Hsun Yang, Yi-Jen Tsai, et al. "Synthesis and Hydrogelation of Star-Shaped Graft Copolypetides with Asymmetric Topology." Gels 8, no. 6 (2022): 366. http://dx.doi.org/10.3390/gels8060366.

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To study the self-assembly and hydrogel formation of the star-shaped graft copolypeptides with asymmetric topology, star-shaped poly(L-lysine) with various arm numbers were synthesized by using asymmetric polyglycerol dendrimers (PGDs) as the initiators and 1,1,3,3-tetramethylguanidine (TMG) as an activator for OH groups, followed by deprotection and grafting with indole or phenyl group on the side chain. The packing of the grafting moiety via non-covalent interactions not only facilitated the polypeptide segments to adopt more ordered conformations but also triggered the spontaneous hydrogela

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Hou, Yong, Meiying Chen, Zhaocui Sun, et al. "The Biosynthesis Related Enzyme, Structure Diversity and Bioactivity Abundance of Indole-Diterpenes: A Review." Molecules 27, no. 20 (2022): 6870. http://dx.doi.org/10.3390/molecules27206870.

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Indole diterpenes are a large class of secondary metabolites produced by fungi, possessing a cyclic diterpenoid backbone and an indole moiety. Novel structures and important biological activity have made indole diterpenes one of the focuses of synthetic chemists. Although the discovery, identification, structural diversity, biological activity and especially structure–activity relationship of indole diterpenes have been reported in some papers in recent years, they are absent of a systematic and comprehensive analysis, and there is no elucidation of enzymes related to this kind of natural prod

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Thomas, Joice, Sampad Jana, Mahendra Sonawane, et al. "A new four-component reaction involving the Michael addition and the Gewald reaction, leading to diverse biologically active 2-aminothiophenes." Organic & Biomolecular Chemistry 15, no. 18 (2017): 3892–900. http://dx.doi.org/10.1039/c7ob00707h.

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A Gewald-four component reaction has been successfully developed for the synthesis of a series of compounds containing an indole and a 2-aminothiophene moiety separated by a methylene spacer having anti-proliferative activity.

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Saad, Hosam A., and Ahmed H. Moustafa. "Synthesis of fused heteropolycyclic systems containing an indole moiety." Journal of Chemical Research 2006, no. 5 (2006): 318–23. http://dx.doi.org/10.3184/030823406777411089.

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Wang, Baolin, Kota Koshino, and Rei Kinjo. "Bicyclic (amino)(borata)carbene derived from diazadiborinine and isonitrile." Chemical Communications 55, no. 86 (2019): 13012–14. http://dx.doi.org/10.1039/c9cc06453b.

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The reaction of 1,4,2,5-diazadiborinine (1) with an aryl isonitrile afforded a bicyclic product containing an indole unit (2) or ketenimine moiety (3), suggesting the generation of a B,N-carbene intermediate formed in the initial step.

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Shehzad, Muhammad Tariq, Ajmal Khan, Sobia Ahsan Halim, et al. "Synthesis of indole-substituted thiosemicarbazones as an aldose reductase inhibitor: an in vitro, selectivity and in silico study." Future Medicinal Chemistry 13, no. 14 (2021): 1185–201. http://dx.doi.org/10.4155/fmc-2020-0060.

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Aim: Indole is an important component of many drug molecules, and its conjugation with thiosemicarbazone moiety would be advantageous in finding lead compounds for the development of diabetic complications. Methodology: We have designed, synthesized and evaluated a series of 17 indole-thiosemicarbazones (3a–q) as aldose reductase (ALR2) and aldehyde reductase (ALR1) inhibitors. Results: After in vitro evaluation, all indole-thiosemicarbazones showed significant inhibition against both enzyme ALR1 and ALR2 with IC50 in range of 0.42–20.7 and 1.02–19.1 μM, respectively. The docking study was als

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Göktaş, Füsun, Gizem Nur Duran, Mehmet Özbil, Özge Soylu-Eter, and Nilgün Karalı. "1H-Indole-2,3-dione 3-thiosemicarbazones Carrying a 4-sulfamoylphenyl Moiety with Selective Antiviral Activity Against Reovirus-1." Acta Chimica Slovenica 71, no. 2 (2024): 215–25. http://dx.doi.org/10.17344/acsi.2023.8589.

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1H-Indole-2,3-dione 3-[4-(4-sulfamoylphenyl)thiosemicarbazones] 6a–j were evaluated against para-influenza-3, reovirus-1, sindbis, coxsackie B4, and Punto Toro viruses. New 1-methyl-1H-indole-2,3-dione 3-[4-(4-sulfamoylphenyl) thiosemicarbazones] 7a–c were synthesized to evaluate the contribution of methyl substitution at position 1 of the indole ring to antiviral activity. The test results showed that 5-trifluoromethoxy substituted compound 6c (EC50 2–9 μM) and 5-bromo substituted 6f (EC50 2–3 μM) have non-toxic selective antiviral activity, while not all standards are active against reovirus

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Sayed, Mostafa, Ahmed M. Sayed, Ahmed A. El-Rashedy, et al. "Anti-inflammatory Activity and Computational Biology Study of Indole/Pyrimidine Hybrids." Current Organic Chemistry 28, no. 1 (2024): 56–64. http://dx.doi.org/10.2174/0113852728289430231227042754.

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Abstract: This research paper embarks on an interdisciplinary exploration encompassing synthetic chemistry, pharmacology, and computational biology. The development of novel anti-inflammatory agents is an imperative endeavor within pharmaceutical research. Pyrimidines and thienopyrimidines are class of heterocyclic compounds that have gained prominence for their diverse pharmacological properties, including potential anti-inflammatory effects. When augmented with an indole moiety, these compounds exhibit structural diversity that can profoundly influence their biological activities. The integr

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Heravi, Majid M., Zahra Amiri, Kosar Kafshdarzadeh, and Vahideh Zadsirjan. "Synthesis of indole derivatives as prevalent moieties present in selected alkaloids." RSC Advances 11, no. 53 (2021): 33540–612. http://dx.doi.org/10.1039/d1ra05972f.

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Bellavita, Rosa, Marcello Casertano, Nicola Grasso, et al. "Microwave-Assisted Synthesis of 2-Methyl-1H-indole-3-carboxylate Derivatives via Pd-Catalyzed Heterocyclization." Symmetry 14, no. 3 (2022): 435. http://dx.doi.org/10.3390/sym14030435.

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Indole moiety is well-known as a superlative framework in many natural products and synthetic pharmaceuticals. Herein, we report an efficient procedure to synthesize a series of functionalized 2-methyl-1H-indole-3-carboxylate derivatives from commercially available anilines properly functionalized by different electron-withdrawing and -donating groups through a palladium-catalyzed intramolecular oxidative coupling. The conversion of a variety of enamines into the relevant indole was optimized by exposing the neat mixture of reactants to microwave irradiation, obtaining the desired products in

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