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Journal articles on the topic 'ACRIDINE SERIES'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Krochtová, Kristína, Annamária Halečková, Ladislav Janovec, Michaela Blizniaková, Katarína Kušnírová, and Mária Kožurková. "Novel 3,9-Disubstituted Acridines with Strong Inhibition Activity against Topoisomerase I: Synthesis, Biological Evaluation and Molecular Docking Study." Molecules 28, no. 3 (2023): 1308. http://dx.doi.org/10.3390/molecules28031308.

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A series of novel 3,9-disubstituted acridines were synthesized and their biological potential was investigated. The synthetic plan consists of eight reaction steps, which produce the final products, derivatives 17a–17j, in a moderate yield. The principles of cheminformatics and computational chemistry were applied in order to study the relationship between the physicochemical properties of the 3,9-disubstituted acridines and their biological activity at a cellular and molecular level. The selected 3,9-disubstituted acridine derivatives were studied in the presence of DNA using spectroscopic (U

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2

Godard, A., P. Rocca, F. Guillier та ін. "Ortho-directed metallation of π-deficient heterocycles in connection with palladium-catalyzed biaryl cross-coupling Synthesis of marine alkaloids of the pyridoacridine series". Canadian Journal of Chemistry 79, № 11 (2001): 1754–61. http://dx.doi.org/10.1139/v01-147.

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Connection between ortho-directed metallation of π-deficient heterocycles and Suzuki cross-coupling reactions provides a very efficient and fruitful strategy to polycyclic molecules of biological interest. The methodology is used to synthesize alkaloids or precursors and analogues of natural compounds of the pyrido[2,3,4-k,l]acridine series.Key words: marine alkaloids, pyrido[2,3,4-k,l]acridines, metallation, cross-coupling.

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3

Di Giorgio, Carole, Florence Delmas, Nathalie Filloux, et al. "In Vitro Activities of 7-Substituted 9-Chloro and 9-Amino-2-Methoxyacridines and Their Bis- and Tetra-Acridine Complexes against Leishmania infantum." Antimicrobial Agents and Chemotherapy 47, no. 1 (2003): 174–80. http://dx.doi.org/10.1128/aac.47.1.174-180.2003.

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ABSTRACT 9-Chloro and 9-amino-2-methoxyacridines bearing different substituents in position 7, as well as their corresponding unsubstituted dimeric and tetrameric complexes, were investigated for in vitro antiproliferative properties against Leishmania infantum compared to toxicity towards human monocytes. The results clearly confirmed that several compounds of the 2-methoxyacridine series, together with their corresponding dimeric and tetrameric derivatives, had strong in vitro antiparasitic properties. Antileishmanial activity was shown to depend on the nature of both 7- and 9-substituted gr

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4

Pravin, R. Kawle, and P. Deohate Pradip. "Synthesis of heterocycles containing pyrimidine-acridine rings by microwave irradiation, antimicrobial study and its comparison with classical heating." Journal of Indian Chemical Society Vol. 92, Jun 2015 (2015): 925–28. https://doi.org/10.5281/zenodo.5637765.

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Department of Chemistry, Shri R. L. T. College of Science, Akola-444 001, Maharashtra, India <em>E-mail</em> : pravink280685@rediffmail.com New series of linked heterocycles containing acridine and pyrimidines were prepared in high yield from condensation of <em>N</em>-acridin-9-yl-3-oxo-butyramide with urea or thiourea or guanidine by microwave irradiation and by conventional heating for comparative study purpose. The representative compounds characterized on the basis of IR, <sup>1</sup>H NMR and Mass spectral beside elemental analysis. Microwave assisted synthesized compounds evaluated for

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5

Sharhan, Olla, Thorsten Heidelberg, Najiahah Mohd Hashim, Abbas Abdulameer Salman, Hapipah Mohd Ali, and Soher Nagi Jayash. "Synthesis and biological study of acridine-based imidazolium salts." RSC Advances 8, no. 68 (2018): 38995–9004. http://dx.doi.org/10.1039/c8ra08138g.

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6

Roe, S., M. Gunaratnam, C. Spiteri, et al. "Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors." Organic & Biomolecular Chemistry 13, no. 31 (2015): 8500–8504. http://dx.doi.org/10.1039/c5ob01177a.

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7

Rosero-Mafla, Miguel A., Jhon Zapata-Rivera, M. Concepción Gimeno, and Renso Visbal. "Steric and Electronic Effects in N-Heterocyclic Carbene Gold(III) Complexes: An Experimental and Computational Study." Molecules 27, no. 23 (2022): 8289. http://dx.doi.org/10.3390/molecules27238289.

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A series of neutral acridine-based gold(III)-NHC complexes containing the pentafluorophenyl (–C6F5) group were synthesized. All of the complexes were fully characterized by analytical techniques. The square planar geometry around the gold center was confirmed by X-ray diffraction analysis for complexes 1 (Trichloro [1-methyl-3-(9-acridine)imidazol-2-ylidene]gold(III)) and 2 (Chloro-bis(pentafluorophenyl)[1-methyl-3-(9-acridine)imidazol-2-ylidene]gold(III)). In both cases, the acridine rings play a key role in the crystal packing of the solid structures by mean of π–π stacking interactions, wit

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8

Potdar, Shweta, Nikita Pal, Pratibha Sharma, and Ashok Kumar. "The catalytic influence of phosphotungstic acid-functionalized Fe3O4 MNPs blended with TiO2 on the synthesis of novel spiro-acridines and the evaluation of their medicinal potential through molecular docking studies." RSC Advances 10, no. 72 (2020): 44442–52. http://dx.doi.org/10.1039/d0ra06975b.

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This manuscript describes an effective and rapid three-component synthesis of a novel series of spiro-acridine derivatives by integrating the pharmacologically dynamic hydantoin–phenytoin as the prime synthetic equivalent.

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9

Druzina, Anna A., Nadezhda V. Dudarova, Ivan V. Ananyev, et al. "New Boron Containing Acridines: Synthesis and Preliminary Biological Study." Molecules 28, no. 18 (2023): 6636. http://dx.doi.org/10.3390/molecules28186636.

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The synthesis of the first conjugates of acridine with cobalt bis(dicarbollide) are reported. A novel 9-azido derivative of acridine was prepared through the reaction of 9-methoxyacridine with N3CH2CH2NH2, and its solid-state molecular structure was determined via single-crystal X-ray diffraction. The azidoacridine was used in a copper (I)-catalyzed azide-alkyne cycloaddition reaction with cobalt bis(dicarbollide)-based terminal alkynes to give the target 1,2,3-triazoles. DNA interaction studies via absorbance spectroscopy showed the weak binding of the obtained conjugates with DNA. The antipr

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10

Piestrzeniewicz, Mariola K., Dorota Wilmańska, Kazimierz Studzian, et al. "Inhibition of RNA Synthesis in vitro by Acridines - Relation between Structure and Activity." Zeitschrift für Naturforschung C 53, no. 5-6 (1998): 359–68. http://dx.doi.org/10.1515/znc-1998-5-610.

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Abstract The effects of acridine derivatives (proflavine and 2,7-dialkyl derivatives, diacridines and triacridines, 9-aminoacridine carboxamides, and 9-anilinoacridine, amsacrine and its congeners) on overall RNA synthesis in vitro, on synthesis of initiating oligonucleotides and the binding of the enzyme to DNA were studied. The primary mechanism of action is related to inhibition of the enzyme binding to DNA. The acridines (intercalating or non-intercalating and bis-intercalating ligands) assayed here differ in the properties of their complexes with DNA. Correlation is generally observed bet

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11

Josephrajan, T., and V. T. Ramakrishnan. "Thermal and microwave assisted synthesis of N-aroylamino acridinediones." Canadian Journal of Chemistry 85, no. 9 (2007): 572–75. http://dx.doi.org/10.1139/v07-075.

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A series of N-aroylamino acridinediones (3a–3d and6a–6e) have been synthesized from tetraketones (1 and 4) and benzoic hydrazides (2a–2d and 5a–5e) under thermal and microwave irradiation conditions with solid supports.Key words: acridine, hydrazide, microwave irradiation.

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12

Csuk, René, Christian Raschke, Gunnar Göthe, and Stefan Reißmann. "Synthesis of Monomeric Acridine Derived Nucleic Acid Intercalators." Zeitschrift für Naturforschung B 60, no. 1 (2005): 83–88. http://dx.doi.org/10.1515/znb-2005-0113.

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A series of antiviral compounds consisting of an intercalating acridine derived part, a spacer region and a reactive EDTA-derived conjugate was synthesized in an easy sequence. In the presence of ascorbate a reduction of the phage-titer of MS2 phages by several logarithmic decades was achieved.

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13

Kowalska, Kornelia, Damian Trzybiński, and Artur Sikorski. "Influence of the halogen substituent on the formation of halogen and hydrogen bonding in co-crystals formed from acridine and benzoic acids." CrystEngComm 17, no. 37 (2015): 7199–212. http://dx.doi.org/10.1039/c5ce01321f.

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A series of nine co-crystals formed from acridine and benzoic acids have been synthesized and structurally characterized and the influence of the halogen substituent on the formation of halogen and hydrogen bonding in the co-crystals of the title compounds has been investigated.

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14

Komatsu, Ryutaro, Hisahiro Sasabe, Yuki Seino, Kohei Nakao, and Junji Kido. "Light-blue thermally activated delayed fluorescent emitters realizing a high external quantum efficiency of 25% and unprecedented low drive voltages in OLEDs." Journal of Materials Chemistry C 4, no. 12 (2016): 2274–78. http://dx.doi.org/10.1039/c5tc04057d.

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A series of TADF emitters composed of pyrimidine/acridine moieties are developed. The optimized device realized its highest power efficiency of 62 lm W<sup>−1</sup>, a high external quantum efficiency of 25%, and a low turn-on voltage of 2.8 V with light-blue emission.

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15

Csuk, René, Thorsten Brezesinski, Gunnar Göthe, Christian Raschke, and Stefan Reißmann. "Synthesis of Dimeric Acridine Derived Nucleic Acid Intercalators." Zeitschrift für Naturforschung B 60, no. 1 (2005): 89–98. http://dx.doi.org/10.1515/znb-2005-0114.

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A series of antiviral compounds consisting of an intercalating acridine derived part, a spacer region and a reactive EDTA-derived conjugate was synthesized in an easy sequence. Suitably monoprotected 1,ω-alkyldiamines gave upon reaction with 6,9-dichloro-2-methoxyacridine (1) followed by deprotection and reaction with EDTA dianhydride the target molecules. In the presence of ascorbate a reduction of the phage-titer of the MS2 phages by > 8 logarithmic decades was achieved.

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16

Sharma, Anamika, Sonika Jain, Reenu Sirohi, and D. Kishore. "Synthesis of [2′-(N-Ethylamino)-5′-Alkyl]phenyl-5,6,7,8-Tetrahydroacridine-9-Carboxy-2-Sulfone Derivatives by the Proton-Catalyzed Rearrangement of Corresponding Sulfonamides." Organic Chemistry International 2011 (January 11, 2011): 1–5. http://dx.doi.org/10.1155/2011/614627.

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Synthesis of a new series of heteroaryl sulfones 6(a–f) in which the heteroaryl part is represented by acridine derivatives has been developed and reported here. The key step of this transformation involves the proton-catalyzed rearrangement of the sulphonamide derivatives 5(a–f) to the corresponding sulfones 6(a–f).

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17

Martano, Marina, Emanuela Morello, Sofia Avnet, et al. "Photodynamic Surgery for Feline Injection-Site Sarcoma." BioMed Research International 2019 (July 8, 2019): 1–9. http://dx.doi.org/10.1155/2019/8275935.

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Musculoskeletal sarcomas are rare and aggressive human malignancies affecting bones and soft tissues with severe consequences, in terms of both morbidity and mortality. An innovative technique that combines photodynamic surgery (PDS) and therapy (PDT) with acridine orange has been recently suggested, showing promising results. However, due to the low incidence of sarcoma in humans, this procedure has been attempted only in pilot studies and stronger evidence is needed. Naturally occurring tumors in cats are well-established and advantageous models for human cancers. Feline injection-site sarco

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18

Joe, Frank L., Jean Salemme, and Thomas Fazio. "Liquid Chromatographic Determination of Basic Nitrogen-Containing Polynuclear Aromatic Hydrocarbons in Smoked Foods." Journal of AOAC INTERNATIONAL 69, no. 2 (1986): 218–22. http://dx.doi.org/10.1093/jaoac/69.2.218.

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Abstract Several smoked foods were analyzed for basic nitrogen-containing polynuclear aromatic hydrocarbon (NPAH) content by a relatively rapid liquid chromatographic (LC) technique. The analyzed products included both domestic and imported market basket commodities. Nanogram quantities of NPAH standards were detected by UV and fluorescence detectors connected in series. The NPAHs were extracted from basic aqueous ethanolic solution into cyclohexane, extracted from cyclohexane into 6N HC1, and extracted back into cyclohexane after neutralization of the acid. The NPAHs were then purified by fil

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19

Huo, Lini, Xiaochen Liu, Yogini Jaiswal, et al. "Design and Synthesis of Acridine-Triazole and Acridine-Thiadiazole Derivatives and Their Inhibitory Effect against Cancer Cells." International Journal of Molecular Sciences 24, no. 1 (2022): 64. http://dx.doi.org/10.3390/ijms24010064.

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We report herein the design and synthesis of a series of novel acridine-triazole and acridine-thiadiazole derivatives. The newly synthesized compounds and the key intermediates were all evaluated for their antitumor activities against human foreskin fibroblasts (HFF), human gastric cancer cells-803 (MGC-803), hepatocellular carcinoma bel-7404 (BEL-7404), large cell lung cancer cells (NCI-H460), and bladder cancer cells (T24). Most of the compounds exhibited high levels of antitumor activity against MGC-803 and T24 but low toxicity against human normal liver cells (LO2), and their effect was ev

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20

Xu, Shengang, Mujie Yang, and Shaokui Cao. "Synthesis and optical properties of two series of soluble acridine-containing copolyimides." Polymer 48, no. 8 (2007): 2241–49. http://dx.doi.org/10.1016/j.polymer.2007.02.046.

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21

Herole R A and Rakesh Kumar Jat. "Synthesis, Characterisation and Anticancer Study of Acridine derivatives." Tropical Journal of Pharmaceutical and Life Sciences 10, no. 5 (2023): 50–56. http://dx.doi.org/10.61280/tjpls.v10i5.146.

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Cancer is one of the global problem and a major cause for mortality. many treatment strategies are available for cancer treatment, still there is a scope for novel treatment to avoid serious side effects of existing therapy. Novel DNA binding agents are needed for effective treatment of cancers. In the field of antitumor DNA-intercalating agents, 9-aminoacridines play an important role due to their antiproliferative properties. Several cancer chemotherapeutics such as amsacrine and nitracrine have been developed as anticancer agents.In present study, a series of new acridine-based derivatives

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22

Csuk, René, Stefan Schwarz, Bianka Siewert, Ralph Kluge, and Dieter Ströhl. "Synthesis and Cytotoxic Activity of Methyl Glycyrrhetinate Esterified with Amino Acids." Zeitschrift für Naturforschung B 67, no. 7 (2012): 731–46. http://dx.doi.org/10.5560/znb.2012-0107.

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Methyl glycyrrhetinate was esterified at position C3 of ring A using different amino acids. A short, unbranched chain of four carbon atoms with two amino groups in positions 2 and 4 was shown to be the most active compound of this series (IC50 = 0:8 M on liposarcoma Lipo cells). These compounds trigger apoptosis as shown by an acridine orange/ethidium bromide assay, trypan blue tests and DNA laddering experiments.

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23

PANDEY, SWAROOP KUMAR, SUBHASISH BISWAS, SARIKA GUNJAN, et al. "Pyrrolidine-Acridine hybrid in Artemisinin-based combination: a pharmacodynamic study." Parasitology 143, no. 11 (2016): 1421–32. http://dx.doi.org/10.1017/s0031182016000937.

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SUMMARYAiming to develop new artemisinin-based combination therapy (ACT) for malaria, antimalarial effect of a new series of pyrrolidine-acridine hybrid in combination with artemisinin derivatives was investigated. Synthesis, antimalarial and cytotoxic evaluation of a series of hybrid of 2-(3-(substitutedbenzyl)pyrrolidin-1-yl)alkanamines and acridine were performed and mode of action of the lead compound was investigated. In vivo pharmacodynamic properties (parasite clearance time, parasite reduction ratio, dose and regimen determination) against multidrug resistant (MDR) rodent malaria paras

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Vilková, Mária, Monika Hudáčová, Nikola Palušeková, et al. "Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties." Molecules 27, no. 9 (2022): 2883. http://dx.doi.org/10.3390/molecules27092883.

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A series of novel acridine N-acylhydrazone derivatives have been synthesized as potential topoisomerase I/II inhibitors, and their binding (calf thymus DNA—ctDNA and human serum albumin—HSA) and biological activities as potential anticancer agents on proliferation of A549 and CCD-18Co have been evaluated. The acridine-DNA complex 3b (-F) displayed the highest Kb value (Kb = 3.18 × 103 M−1). The HSA-derivatives interactions were studied by fluorescence quenching spectra. This method was used for the calculation of characteristic binding parameters. In the presence of warfarin, the binding const

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Mattioda, A. L., C. W. Bauschlicher, A. Ricca, J. Bregman, D. M. Hudgins, and L. J. Allamandola. "Infrared spectroscopy of matrix-isolated neutral polycyclic aromatic nitrogen heterocycles: The acridine series." Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 181 (June 2017): 286–308. http://dx.doi.org/10.1016/j.saa.2017.03.044.

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26

Edward Lindsell, W., Christopher Murray, Peter N. Preston, and Thomas A. J. Woodman. "Synthesis of 1,3-Diynes in the Purine, Pyrimidine, 1,3,5-Triazine and Acridine Series." Tetrahedron 56, no. 9 (2000): 1233–45. http://dx.doi.org/10.1016/s0040-4020(00)00016-8.

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27

Vlassa, M., and Maria Kezdi. "Application of phase transfer catalysis in the acridine series. V. Synthesis of Thioacridones." Journal f�r Praktische Chemie 329, no. 1 (1987): 141–44. http://dx.doi.org/10.1002/prac.19873290121.

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28

Wei, Ying, Lei Tang, Chunxiao Zhong, et al. "Photooxygenations and Self-Sensitizations of Naphthylamines: Efficient Access to Iminoquinones." Journal of Chemistry 2018 (2018): 1–9. http://dx.doi.org/10.1155/2018/9180671.

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A series of spiro [fluorene-9,7′-dibenzo[c,h]acridine]-5′-one (SFDBAO) derivatives have been concisely and cleanly obtained by exposure to sunlight without external photosensitizers in the higher yields than that when using a UV lamp. An interesting autocatalyst and self-sensitive procedure have been proposed to explain the effective photooxygenation. SFDBAO derivatives exhibit the continuous π-stacks in single-crystal and electron-withdraw properties with red light-emitting and photovoltaic properties.

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Almasirad, Ali, Loghman Firoozpour, Maliheh Nejati, et al. "Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents." Zeitschrift für Naturforschung B 71, no. 3 (2016): 205–10. http://dx.doi.org/10.1515/znb-2015-0138.

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AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

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R, Kalirajan. "Microwave Irradated Synthesis, Characterization and Evaluation for their Antibacterial and Larvicidal Activities of some Novel Chalcone and Isoxazole Substituted 9-Anilino Acridines." Open Journal of Chemistry 1, no. 1 (2015): 001–7. https://doi.org/10.17352/ojc.000001.

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<strong>Introduction:</strong> Chalcone, isoxazole and acridines have diverse biological activities. A series of novel chalcone and isoxazole substituted 9-anilinoacridines were synthesized for their antibacterial, larvicidal, activities. <strong>Methods: </strong>A series of novel chalcone and isoxazole substituted 9-anilinoacridines (3a-h and 4a-h) were synthesized from 9-chloroacridine by microwave irradiation method. The antibacterial evaluation was performed by cup-plate method and screened for their larvicidal activity by larval bioassay method. Result: The compounds 3d, 3e, 3f, 3h, 4d,

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Friedel, Joshua, Maren Krause, Rose Jordan, et al. "Triplet Emitting C^N^C Cyclometalated Dibenzo[c,h]Acridine Pt(II) Complexes." Molecules 27, no. 22 (2022): 8054. http://dx.doi.org/10.3390/molecules27228054.

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In a series of Pt(II) complexes [Pt(dba)(L)] containing the very rigid, dianionic, bis-cyclometalating, tridentate C^N^C2− heterocyclic ligand dba2– (H2dba = dibenzo[c,h]acridine), the coligand (ancillary ligand) L = dmso, PPh3, CNtBu and Me2Imd (N,N’-dimethylimidazolydene) was varied in order to improve its luminescence properties. Beginning with the previously reported dmso complex, we synthesized the PPh3, CNtBu and Me2Imd derivatives and characterized them by elemental analysis, 1H (and 31P) NMR spectroscopy and MS. Cyclic voltammetry showed partially reversible reduction waves ranging bet

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Kadutskii, A. P., N. G. Kozlov, and S. L. Bondarev. "Crotonization in the benzo[a]acridine series. Synthesis of naphtho[2,1-j][1,7]phenanthroline derivatives." Russian Journal of Organic Chemistry 42, no. 9 (2006): 1383–87. http://dx.doi.org/10.1134/s1070428006090235.

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Lindsell, W. Edward, Christopher Murray, Peter N. Preston, and Thomas A. J. Woodman. "ChemInform Abstract: Synthesis of 1,3-Diynes in the Purine, Pyrimidine, 1,3,5-Triazine and Acridine Series." ChemInform 31, no. 19 (2010): no. http://dx.doi.org/10.1002/chin.200019091.

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Danihel, Ivan, Ján Imrich, Pavol Kristian, Tibor Liptaj, and Dana Mazagová. "An Analysis of Substituent Effects on the Proton and Carbon-13 Chemical Shifts of 2-Substituted 9-Isothiocyanatoacridines." Collection of Czechoslovak Chemical Communications 59, no. 8 (1994): 1833–40. http://dx.doi.org/10.1135/cccc19941833.

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Proton and 13C NMR chemical shifts and coupling constants J(H,H) of a series of 2-substituted 9-isothiocyanatoacridines and their 4-methyl and 4-methoxy analogs were determined. The obtained values were utilized in analysis of substituent effects using empirical equations based on two- and three-parameter linear correlations. It was found that short-range interactions (positions ipso, ortho and meta) are well described by the three-parameter model of Reynolds whereas long-range effects are satisfactorily compatible with the two-parameter model. The dominant direction of conjugation in the acri

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Auparakkitanon, Saranya, Wilai Noonpakdee, Raymond K. Ralph, William A. Denny, and Prapon Wilairat. "Antimalarial 9-Anilinoacridine Compounds Directed at Hematin." Antimicrobial Agents and Chemotherapy 47, no. 12 (2003): 3708–12. http://dx.doi.org/10.1128/aac.47.12.3708-3712.2003.

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ABSTRACT Antimalarial 9-anilinoacridines are potent inhibitors of parasite DNA topoisomerase II both in vitro and in situ. 3,6-Diamino substitution on the acridine ring greatly improves parasiticidal activity against Plasmodium falciparum by targeting DNA topoisomerase II. A series of 9-anilinoacridines were investigated for their abilities to inhibitβ -hematin formation, to form drug-hematin complexes, and to enhance hematin-induced lysis of red blood cells. Inhibition ofβ -hematin formation was minimal with 3,6-diamino analogs of 9-anilinoacridine and greatest with analogs with a 3,6-diCl su

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AITKEN, Jacqueline F., Kerry M. LOOMES, Barbara KONARKOWSKA, and Garth J. S. COOPER. "Suppression by polycyclic compounds of the conversion of human amylin into insoluble amyloid." Biochemical Journal 374, no. 3 (2003): 779–84. http://dx.doi.org/10.1042/bj20030422.

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There is a significant correlation between the occurrence of pancreatic islet amyloid and β-cell failure in advanced type II diabetes mellitus. Islet amyloid is composed primarily of the fibrillar form of the pancreatic hormone, amylin. Using thioflavin-T fluorescence binding and radioprecipitation assays, we investigated whether or not a series of small tricyclic compounds, tetracycline or Congo Red could interfere with the conversion of synthetic human amylin into its insoluble amyloid form. Of the compounds investigated, incubation of human amylin with a 20-fold molar excess of either Congo

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Sarnat, Harvey B., Bernadette Curry, N. B. Rewcastle, and Cynthia L. Trevenen. "Cytoplasmic RNA in Nervous System Tumours in Children: A Fluorochromic Histochemical Study using Acridine Orange." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 13, no. 1 (1986): 31–41. http://dx.doi.org/10.1017/s0317167100035769.

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ABSTRACT:Acridine orange was used as a fluorochromic histochemical stain of nucleic acids, applied to 78 neoplasms of the central and peripheral nervous systems of 60 children. Some cases were compared with 5 adults and 4 other cases of chronic reactive gemistocytic gliosis. Opposite concentration gradients of cytoplasmic ribonucleic acid (RNA) was demonstrated in tumours of the neuronal/neuroectodermal series, and those of the glial/neuroepithelial series. Minimal AO-RNA fluorescence was seen in 8 cerebellar medulloblastomas and in a retinoblastoma; strong AO-RNA fluorescence occurred in one

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Lown, J. William, Sham M. Sondhi, Chi Wi Ong, Andrew Skorobogaty, Hiroko Kishikawa, and James C. Dabrowiak. "Deoxyribonucleic acid cleavage specificity of a series of acridine- and acodazole-iron porphyrins as functional bleomycin models." Biochemistry 25, no. 18 (1986): 5111–17. http://dx.doi.org/10.1021/bi00366a020.

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Maciejewska, Karolina, Kamila Czarnecka, Paweł Kręcisz, et al. "Novel Cyclopentaquinoline and Acridine Analogs as Multifunctional, Potent Drug Candidates in Alzheimer’s Disease." International Journal of Molecular Sciences 23, no. 11 (2022): 5876. http://dx.doi.org/10.3390/ijms23115876.

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A series of new cyclopentaquinoline derivatives with 9-acridinecarboxylic acid and a different alkyl chain length were synthesized, and their ability to inhibit cholinesterases was evaluated. All designed compounds, except derivative 3f, exhibited a selectivity for butyrylcholinesterase (BuChE) with IC50 values ranging from 103 to 539 nM. The 3b derivative revealed the highest inhibitory activity towards BuChE (IC50 = 103.73 nM) and a suitable activity against AChE (IC50 = 272.33 nM). The 3f derivative was the most active compound to AChE (IC50 = 113.34 nM) with satisfactory activity towards B

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Bharathi, A., Selvaraj Mohana Roopan, Abdul Abdul Rahuman, and Govindasamy Rajakumar. "In VitroLarvicidal and Antioxidant Activity of Dihydrophenanthroline-3-carbonitriles." BioMed Research International 2014 (2014): 1–8. http://dx.doi.org/10.1155/2014/915797.

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Many naturally occurring and synthetic compounds containing dihydrocyanopyridine and cyanopyran moiety show pharmacological properties. The aim of this study is to investigate the larvicidal and antioxidant potential of dihydrophenanthroline-3-carbonitrile derivatives4a–f. A novel series of 2-amino-10-chloro-4,12-diphenyl-1,4,5,6-tetrahydrobenzo[j][1,7]phenanthroline-3-carbonitrile derivatives were synthesized by reacting different substituted acridine chalcones through Michel addition. The compounds were synthesized in excellent yields and the structures were corroborated on the basis of FT-I

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Bouchikhi, Nouria, Manel Bouazza, Salah Hamri, et al. "Photo-curing kinetics of hydroxyethyl acrylate (HEA): synergetic effect of dye/amine photoinitiator systems." International Journal of Industrial Chemistry 11, no. 1 (2019): 1–9. http://dx.doi.org/10.1007/s40090-019-00197-7.

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AbstractThe aim of this study is to examine and evaluate several dye/amine systems as photoinitiators for photopolymerization of 2-hydroxyethyl acrylate (HEA) monomer under visible light conditions. For this purpose, a series of dye/amine photoinitiators were formed using methylene blue (MB) or acridine orange (AO) as photosensitizers, and triethanolamine (TEOA), ethyl 4-(dimethylamino) benzoate (EDMAB), trioctylamine (TOA), and N,N-diméthylallylamine (DMAA) as co-initiators. The photopolymerization kinetic of the HEA monomer in the presence of proposed dye/amine systems was performed using Fo

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Jazi, Niloofar, Samieh Fozooni, and Hooshang Hamidian. "One-pot, Multicomponent Synthesis under Microwave Conditions of New Imidazole and Acridine Benzamido Acetic Acid Derivatives." Journal of Chemical Research 42, no. 2 (2018): 80–85. http://dx.doi.org/10.3184/174751918x15181752711035.

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Starting from 4-aminohippuric acid (AHA), two novel series of heterocyclic compounds of pharmaceutical interest have been synthesised by one-pot, multicomponent reactions under microwave conditions. Reaction of AHA with various aldehydes and benzil in (1:1) EtOH/acetic acid in the presence of ammonium acetate yielded 1,2,3,5-tetra-arylated imidazole derivatives, whereas a solvent-free reaction of AHA with various aldehydes and dimedone (2 equiv.) in the presence of p-TSA yielded 4,9-diarylated 1,8-dioxo-decahydroacridine derivatives. These reactions produced good yields in short reaction times

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Vlassa, M., Maria Kezdi, and M. Bogdan. "Applications of phase transfer catalysis in the acridine series. IV. Reactions of 9-Chloroacridine Derivatives with Thiocyanate Ion." Journal f�r Praktische Chemie 327, no. 6 (1985): 1007–10. http://dx.doi.org/10.1002/prac.19853270618.

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VLASSA, M., C. MOLNARIU, and I. A. SILBERG. "ChemInform Abstract: Application of Phase-Transfer Catalysis in Acridine Series. Part 6. Preparation of Some 9-Vinylacridine Derivatives." ChemInform 26, no. 5 (2010): no. http://dx.doi.org/10.1002/chin.199505172.

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Vlassa, M., and Maria Kezdi. "Applications of Phase Transfer Catalysis in the Acridine Series. III. A Simple and Convenient Synthesis of 9-Aminoacridine Derivatives." Journal f�r Praktische Chemie 327, no. 3 (1985): 521–22. http://dx.doi.org/10.1002/prac.19853270319.

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Hassan, Khalid, El-khabiry Shaban, Ghada M. ElHaddad, Asmaa B. Sallam, and Ibrahim El Sayed. "Synthesis, characterization, and antibacterial activity of azodyes incorporated acridine chromophore and their applications in polyester printing." Current Chemistry Letters 11, no. 1 (2022): 83–94. http://dx.doi.org/10.5267/j.ccl.2021.9.002.

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A series of azo dyes incorporated acridine chromophore labelled as 8 (a-d), 10 (a, b), 12 and 14 were prepared in very good yields starting from 9-chloroacridine 1 followed by amination, diazotization and coupling either with rhodanine analogues 6 (a, b) or other coupling partners 9 (a, b), 11 and 13. FT-IR, 1H NMR, and mass spectroscopic analysis were used to establish the structures of the produced azo dispersed dyes. Moreover, the synthesized azo dyes were used to prepare pastes that were used to print polyester fabric using classic silk-screen printing techniques. The dyes were tested for

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Rupar, Jelena, Vladimir Dobričić, Jelena Grahovac, et al. "Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives." RSC Med Chem 11, no. 3 (2020): 378–86. https://doi.org/10.1039/c9md00597h.

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A series of eleven 9-acridinyl amino acid derivatives were synthesized using a two-step procedure. Cytotoxicity was tested on the K562 and A549 cancer cell lines and normal diploid cell line MRC5 using the MTT assay. Compounds 6, 7, 8 and 9 were the most active, with IC50 values comparable to or lower than that of chemotherapeutic agent amsacrine. 8 and 9 were especially effective in the A549 cell line (IC50 ≈ 6 μM), which is of special interest since amsacrine is not sufficiently active in lung cancer patients. Cell cycle analysis revealed that 7 and 9 caused G2/M block, amsacrine ca

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Khalili, Faeze, Sara Akrami, Malihe Safavi, et al. "Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents." Anti-Cancer Agents in Medicinal Chemistry 19, no. 2 (2019): 265–75. http://dx.doi.org/10.2174/1871520618666180903100835.

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Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated b

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Martens-Habbena, Willm, and Henrik Sass. "Sensitive Determination of Microbial Growth by Nucleic Acid Staining in Aqueous Suspension." Applied and Environmental Microbiology 72, no. 1 (2006): 87–95. http://dx.doi.org/10.1128/aem.72.1.87-95.2006.

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ABSTRACT The determination of cell numbers or biomass in laboratory cultures or environmental samples is usually based on turbidity measurements, viable counts, biochemical determinations (e.g., protein and lipid measurements), microscopic counting, or recently, flow cytometric analysis. In the present study, we developed a novel procedure for the sensitive quantification of microbial cells in cultures and most-probable-number series. The assay combines fluorescent nucleic acid staining and subsequent fluorescence measurement in suspension. Six different fluorescent dyes (acridine orange, DAPI

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Neves, Ana Rita, Fernando Durães, Joana Freitas-Silva, et al. "Derivatives of Trimethoxybenzoic Acid and Gallic Acid as Potential Efflux Pump Inhibitors: In Silico and In Vitro Studies." International Journal of Molecular Sciences 23, no. 22 (2022): 14468. http://dx.doi.org/10.3390/ijms232214468.

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The overexpression of efflux pumps is one of the strategies used by bacteria to resist antibiotics and could be targeted to circumvent the antibiotic crisis. In this work, a series of trimethoxybenzoic acid derivatives previously described as antifouling compounds was explored for potential antimicrobial activity and efflux pump (EP) inhibition. First, docking studies on the acridine resistance proteins A and B coupled to the outer membrane channel TolC (AcrAB-TolC) efflux system and a homology model of the quinolone resistance protein NorA EP were performed on 11 potential bioactive trimethox

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