Academic literature on the topic 'Antimitotic Activity'

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Journal articles on the topic "Antimitotic Activity"

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Sundaresan, K., M. Thangavel, and K. Tharini. "Synthesis, characterization and antimitotic activity of N-benzyl piperidin 4-one oxime." Journal of Drug Delivery and Therapeutics 9, no. 1 (2019): 233–36. http://dx.doi.org/10.22270/jddt.v9i1.2228.

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The aim of this study was to synthesize, characterization and antimitotic activity of N-Benzyl piperidin 4-one oxime derivative. The synthesized compound was characterized by IR, 13C and 1H NMR spectral studies. The synthesized compound was subjected to antimitotic studies of alliumcepa root meristamatic cells. The mitotic activity was observed in 3 different concentrations of N-Benzyl piperidin 4-one oxime. Our findings support the reported therapeutic use of this compound as a antimitotic or anticancer agent in the Indian system of medicine.
 Keywords: N-Benzyl piperidin 4-one oxime, meristamatic cells, mitotic index.
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R. A. Ahirrao, B. S. Patange, and S. V. More. "Evaluation of Antimitotic Activity of Momordica Dioica Fruits on Allium Cepa Root Meristamatic Cells." Journal of Pharmaceutical Technology, Research and Management 7, no. 2 (2019): 67–71. http://dx.doi.org/10.15415/jptrm.2019.72009.

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Objective: Natural occurring phenolic compounds play an important role in cancer prevention and shows antimitotic activity. Number of active constituents like phenolic acid, curcuminoids, coumarine, ligans, quinones, etc. is showing antimitotic activity of Momordica dioica. The present work is on phytochemical investigation and examines antimitotic activity of aqueous extract of fruits Momordica dioica at concentration of 15 mg/ml on Allium cepa root meristamatic cells.Methods: The fruits are air dried and extracted with solvents like water by maceration method. The evaluation of antimitotic activity is done by using Allium cepa root meristamatic cells parameters where and methotrexate was used as a standard drugs. Result and discussion: In Allium assay, aqueous extract of fruits of Momordica diocia (15 mg/ml) and methotrexate act against cells of allium roots and lesser the growth of root and mitotic index when compared with distilled water as control group. The result indicated that cytotoxic property is due to presence of phenolic, alkaloids and flavonoids compounds in 15 mg/ml concentration of aqueous extract of Momordica diocia fruits extract.Conclusion: On the basis of result, we concluded that, 15 mg/ml concentration of Momordica dioica fruits shows good antimitotic activity on the Allium cepa root tip assay.
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Groult, Hugo, Isabel García-Álvarez, Lorenzo Romero-Ramírez, et al. "Micellar Iron Oxide Nanoparticles Coated with Anti-Tumor Glycosides." Nanomaterials 8, no. 8 (2018): 567. http://dx.doi.org/10.3390/nano8080567.

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The synthesis procedure of nanoparticles based on thermal degradation produces organic solvent dispersible iron oxide nanoparticles (OA-IONP) with oleic acid coating and unique physicochemical properties of the core. Some glycosides with hydrophilic sugar moieties bound to oleyl hydrophobic chains have antimitotic activity on cancer cells but reduced in vivo applications because of the intrinsic low solubility in physiological media, and are prone to enzymatic hydrolysis. In this manuscript, we have synthetized and characterized OA-IONP-based micelles encapsulated within amphiphilic bioactive glycosides. The glycoside-coated IONP micelles were tested as Magnetic Resonance Imaging (MRI) contrast agents as well as antimitotics on rat glioma (C6) and human lung carcinoma (A549) cell lines. Micelle antimitotic activity was compared with the activity of the corresponding free glycosides. In general, all OA-IONP-based micellar formulations of these glycosides maintained their anti-tumor effects, and, in one case, showed an unusual therapeutic improvement. Finally, the micelles presented optimal relaxometric properties for their use as T2-weighed MRI contrast agents. Our results suggest that these bioactive hydrophilic nano-formulations are theranostic agents with synergistic properties obtained from two entities, which separately are not ready for in vivo applications, and strengthen the possibility of using biomolecules as both a coating for OA-IONP micellar stabilization and as drugs for therapy.
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Badria, Farid A., Waell E. Houssein, Mona G. Zaghloul, and Ahmed F. Halim. "Antimitotic Activity of Gossypol and Gossypolone." Pharmaceutical Biology 39, no. 2 (2001): 120–26. http://dx.doi.org/10.1076/phbi.39.2.120.6257.

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Zhai, Lei, Anushree Balachandran, Rebecca Larkin, et al. "Mitotic Dysregulation at Tumor Initiation Creates a Therapeutic Vulnerability to Combination Anti-Mitotic and Pro-Apoptotic Agents for MYCN-Driven Neuroblastoma." International Journal of Molecular Sciences 24, no. 21 (2023): 15571. http://dx.doi.org/10.3390/ijms242115571.

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MYCN amplification occurs in approximately 20–30% of neuroblastoma patients and correlates with poor prognosis. The TH-MYCN transgenic mouse model mimics the development of human high-risk neuroblastoma and provides strong evidence for the oncogenic function of MYCN. In this study, we identified mitotic dysregulation as a hallmark of tumor initiation in the pre-cancerous ganglia from TH-MYCN mice that persists through tumor progression. Single-cell quantitative-PCR of coeliac ganglia from 10-day-old TH-MYCN mice revealed overexpression of mitotic genes in a subpopulation of premalignant neuroblasts at a level similar to single cells derived from established tumors. Prophylactic treatment using antimitotic agents barasertib and vincristine significantly delayed the onset of tumor formation, reduced pre-malignant neuroblast hyperplasia, and prolonged survival in TH-MYCN mice. Analysis of human neuroblastoma tumor cohorts showed a strong correlation between dysregulated mitosis and features of MYCN amplification, such as MYC(N) transcriptional activity, poor overall survival, and other clinical predictors of aggressive disease. To explore the therapeutic potential of targeting mitotic dysregulation, we showed that genetic and chemical inhibition of mitosis led to selective cell death in neuroblastoma cell lines with MYCN over-expression. Moreover, combination therapy with antimitotic compounds and BCL2 inhibitors exploited mitotic stress induced by antimitotics and was synergistically toxic to neuroblastoma cell lines. These results collectively suggest that mitotic dysregulation is a key component of tumorigenesis in early neuroblasts, which can be inhibited by the combination of antimitotic compounds and pro-apoptotic compounds in MYCN-driven neuroblastoma.
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Mohan, Gottumukkala Krishna, Malavika Yadav, M. Sandhya Rani, and Kalakotla Shanker. "Antimitotic activity of Borassus flabellifer Seed Coat." Research Journal of Pharmacognosy and Phytochemistry 8, no. 4 (2016): 223. http://dx.doi.org/10.5958/0975-4385.2016.00033.9.

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Satish, Ponnada* Bhagyalaxmi Suvvari. "Synthesis And Antimitotic Activity of Benzotriazole Compound." International Journal of Pharmaceutical Sciences 3, no. 4 (2025): 2932–37. https://doi.org/10.5281/zenodo.15273474.

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The present work to Synthesize benzotriazole Nucleus and study the biological activity of Antimitotic method through by seed germination assay by using the green gram seeds. It is preliminary screening method to identify this benzotriazole basic nucleus is having Anticancer property. By using this seed germination assay method be can studied that this nucleus is having inhibition of seed germination Activity.
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Ramos, Sergio, Alba Vicente-Blázquez, Marta López-Rubio, Laura Gallego-Yerga, Raquel Álvarez, and Rafael Peláez. "Frentizole, a Nontoxic Immunosuppressive Drug, and Its Analogs Display Antitumor Activity via Tubulin Inhibition." International Journal of Molecular Sciences 24, no. 24 (2023): 17474. http://dx.doi.org/10.3390/ijms242417474.

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Antimitotic agents are one of the more successful types of anticancer drugs, but they suffer from toxicity and resistance. The application of approved drugs to new indications (i.e., drug repurposing) is a promising strategy for the development of new drugs. It relies on finding pattern similarities: drug effects to other drugs or conditions, similar toxicities, or structural similarity. Here, we recursively searched a database of approved drugs for structural similarity to several antimitotic agents binding to a specific site of tubulin, with the expectation of finding structures that could fit in it. These searches repeatedly retrieved frentizole, an approved nontoxic anti-inflammatory drug, thus indicating that it might behave as an antimitotic drug devoid of the undesired toxic effects. We also show that the usual repurposing approach to searching for targets of frentizole failed in most cases to find such a relationship. We synthesized frentizole and a series of analogs to assay them as antimitotic agents and found antiproliferative activity against HeLa tumor cells, inhibition of microtubule formation within cells, and arrest at the G2/M phases of the cell cycle, phenotypes that agree with binding to tubulin as the mechanism of action. The docking studies suggest binding at the colchicine site in different modes. These results support the repurposing of frentizole for cancer treatment, especially for glioblastoma.
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Podila, Naresh, Mithun Rudrapal, Subramanyam Sibbala, et al. "In vitro antimitotic activity and in silico study of some 6-fluoro-triazolo-benzothiazole analogues." Pharmacia 70, no. (4) (2023): 887–94. https://doi.org/10.3897/pharmacia.70.e109898.

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In this work, nine 6-fluoro-triazolo-benzothiazole derivatives were prepared and evaluated for in vitro antimitotic activity. In addition, in silico study was also done using tubulin protein (PDB: 6QQN) by molecular docking method. Results revealed that TZ2 and TZ9 were the most active compounds with antimitotic action opposing the standard drug, aspirin. Results of molecular docking exhibited the inhibitory potential of triazolo-benzothiazole against tubulin protein. The mitotic study indicates the efficacy of triazolo-benzothiazole analogues in inhibiting the proliferation of cancer cells either by promoting microtubule formation or affecting microtubules, thereby preventing microtubule breakdown.
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Reethu Metilda Manukonda and Satapathy Dhabal. "Phytochemical Analysis and Evaluation of In Vitro Antimitotic Activity of Allamanda cathartica Methanolic Extract." Journal of Pharma Insights and Research 2, no. 4 (2024): 146–54. http://dx.doi.org/10.69613/92x5vg75.

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Allamanda cathartica, a perennial shrub of the Apocynaceae family, has garnered significant attention in pharmacological research due to its diverse bioactive compounds and potential therapeutic applications. This study aimed to investigate the phytochemical composition and evaluate the in vitro antimitotic activity of A. cathartica methanolic extract. Comprehensive phytochemical screening revealed the presence of carbohydrates, alkaloids, saponin glycosides, proteins, tannins, flavonoids, and amino acids in the extract. The antimitotic potential was assessed using a seed germination assay with Vigna radiata L. (green gram) seeds. The methanolic extract exhibited dose-dependent growth inhibition, with 100 μg/mL concentration demonstrating complete inhibition comparable to the standard drug methotrexate. At lower concentrations of 25 μg/mL and 50 μg/mL, the extract showed 50% and 65.5% inhibition, respectively. These findings suggest that A. cathartica possesses significant antimitotic properties, potentially attributable to its rich phytochemical profile. The study also highlights the plant's other pharmacological activities, including antioxidant, anti-inflammatory, wound healing, and antimicrobial properties. Given the growing interest in natural products for cancer therapeutics, A. cathartica presents a promising candidate for further investigation
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Dissertations / Theses on the topic "Antimitotic Activity"

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Bortolozzi, Roberta. "Study of the mechanism of action of new molecules endowed with antitumoral activity." Doctoral thesis, Università degli studi di Padova, 2012. http://hdl.handle.net/11577/3422142.

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The microtubule system of eukaryotic cells is a critical element in a variety of fundamental cellular processes such as cell proliferation, mitotic spindle formation, maintenance of cell shape, regulation of motility, cell signaling, secretion, and intracellular transport. The important role of microtubules dynamic in mitosis progression and thus in cell proliferation, made them an attractive target for cancer therapy. Many chemically diverse compounds bind and affect tubulin-microtubule system, altering polymerization and dynamics during the particularly vulnerable mitotic stage of the cell cycle, causing alteration in the spindle organization with a delay or block at the metaphase-anaphase transition during mitosis. In this study we evaluated the antiproliferative activity of seven series of novel tubulin polymerization inhibitors deriving from three classes of colchicine site binders: combretastatin-A4, chalcones and pyrroloquinolinones. Furthermore we investigated on the inhibitory effects on tubulin polimerization, cell cycle alteration, and apoptosis induction in in vitro and in vivo models and described a possible mechanism of action. The studied compounds, showed antiproliferative activity derived from a interference with microtubule assembly similar or higher than the reference compounds. As general mechanisms of action, the interaction of such compounds with tubulin, induces cell cycle arrest in the G2/M phase, with increased expression of cyclin B1 and phosphorylation of cdc25c, that trigger to apoptosis in a time- and concentration-dependent manner with activation of caspase-3 and cleavage of PARP and reduction of Bcl-2 prosurvival protein. Moreover, several compounds was effective against cancer cell lines, characterized by high expression of glycoprotein-P and multidrug resistance-associated protein, resistant to chemotherapy drugs such as vinblastine, doxorubucine and taxol. Prelimary experiment carried out in vivo models of tumor xenograft showed a significative reduction of tumor growth suggesting a potential clinical applications for these compounds.<br>Nelle cellule eucariotiche i microtubuli costituiscono un elemento cruciale nella regolazione di molteplici processi cellulari, tra cui la proliferazione, la formazione del fuso mitotico, il mantenimento della forma cellulare, la regolazione della motilità, il signaling cellulare, i processi di secrezione e trasporto intracellulare. Il ruolo fondamentale di tale struttura citoscheletrica nella progressione mitotica e di conseguenza nella proliferazione cellulare rende i microtubuli un ottimo target per la terapia antitumorale. Molti composti aventi struttura chimica differente sono in grado di legare il sistema tubulina-microtubuli, alterandone la polimerizzazione e la dinamica, in particolare durante la fase mitotica del ciclo cellulare, destabilizzando l'organizzazione del fuso mitotico, ritardando o bloccando la transizione metafase-anafase. In questo studio è stata valutata l'attività antiproliferativa di sette serie di nuovi inibitori della polimerizzazione della tubulina, derivati da 3 classi di composti che legano i microtubuli a livello del sito di legame della colchicina: combretastatina-A4, calconi e pirrolochinolinoni. In particolare, è stato studiato in modelli in vitro e in vivo l'effetto di tali inibitori sulla polimerizzazione della tubulina, sul ciclo cellulare e sull'attivazione dell'apoptosi per la descrizione di un possibile meccanismo d'azione. I composti testati hanno mostrato attività antiproliferativa comparabile o superiore rispetto ai composti di riferimento. Per quanto riguarda il meccanismo d'azione, in generale, l'interazione di tali composti con la tubulina induce un blocco del ciclo cellulare in fase G2/M con l'aumento dell'espressione della ciclina B1 e la fosforilazione di Cdc25c. Tale arresto della progressione mitotica porta all'attivazione del processo apoptotico in modo tempo- e concentrazione- dipendente con la attivazione di caspase-3, il taglio proteolitico di PARP e la riduzione delle proteine Bcl-2 antiapoptotiche. Inoltre, alcuni composti hanno mostrato elevata efficacia nell'indurre citotossicità in cellule tumorali multidrug resistant, esprimenti la licoproteina-P e le pompe di efflusso MDR, resistenti a chemioterapici quali vinblastina, doxorubucina e tassolo. Esperimenti preliminari, svolti in modelli murini di xenotrapianto, hanno mostrato una significativa riduzione della crescita tumorale, suggerendo una possibile applicazione clinica per alcuni dei composti studiati.
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Radhakrishna, P. M. "Studies in the synthesis and antimitotic activity of Aza and other analogues of Beta-Apopicropodophyllin." Thesis, 1990. http://hdl.handle.net/2009/2551.

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Teesdale-Spittle, P. H., Klaus Pors, R. Brown, Laurence H. Patterson, and J. A. Plumb. "Development of nonsymmetrical 1,4-disubstituted anthraquinones that are potently active against cisplatin-resistant ovarian cancer cells." 2005. http://hdl.handle.net/10454/3191.

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No<br>A novel series of 1,4-disubstituted aminoanthraquinones were prepared by ipso-displacement of 1,4-difluoro-5,8-dihydroxyanthraquinones by hydroxylated piperidinyl- or pyrrolidinylalkyl-amino side chains. One aminoanthraquinone (13) was further derivatized to a chloropropyl-amino analogue by treatment with triphenylphosphine-carbon tetrachloride. The compounds were evaluated in the A2780 ovarian cancer cell line and its cisplatin-resistant variants (A2780/ cp70 and A2780/MCP1). The novel anthraquinones were shown to possess up to 5-fold increased potency against the cisplatin-resistant cells compared to the wild-type cells. Growth curve analysis of the hydroxyethylaminoanthraquinone 8 in the osteosarcoma cell line U-2 OS showed that the cell cycle is not frozen, rather there is a late cell cycle arrest consistent with the action of a DNA-damaging topoisomerase II inhibitor. Accumulative apoptotic events, using time lapse photography, indicate that 8 is capable of fully engaging cell cycle arrest pathways in G2 in the absence of early apoptotic commitment. 8 and its chloropropyl analogue 13 retained significant activity against human A2780/cp70 xenografted tumors in mice.
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Book chapters on the topic "Antimitotic Activity"

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Commerçon, A., J. D. Bourzat, E. Didier, and François Lavelle. "Practical Semisynthesis and Antimitotic Activity of Docetaxel and Side-Chain Analogues." In ACS Symposium Series. American Chemical Society, 1994. http://dx.doi.org/10.1021/bk-1995-0583.ch017.

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Shih, Chuan, Rima S. Al-Awar, Andrew H. Fray, et al. "Synthesis and Structure-Activity Relationship Studies of Cryptophycins: A Novel Class of Potent Antimitotic Antitumor Depsipeptides." In Anticancer Agents. American Chemical Society, 2001. http://dx.doi.org/10.1021/bk-2001-0796.ch010.

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Madhuri, M. Lakshmi, N. V. L. Suvarchala Reddy V, M. Mamatha, and Syed Sara Afreen. "ANTIPROLIFERATIVE ACTIVITY AND MOLECULAR DOCKING STUDIES OF PHYTOCONSTITUENTS FROM SYZYGIUM ALTERNIFOLIUM BARK." In Futuristic Trends in Pharmacy & Nursing Volume 3 Book 15. Iterative International Publishers, Selfypage Developers Pvt Ltd, 2024. http://dx.doi.org/10.58532/v3bapn15p6ch2.

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The present study carried out to investigate the in vitro antimitotic activity using Allium cepa root tip assay to examine the anticancer potential of Syzygium alternifolium. The phytoconstituents previously determined were subjected to molecular docking studies against Bcl-2 and VEGFR-2 protein as a target receptor to support anticancer activities. Methanolic extract of Syzygium alternifoliumshowed significant antimitotic activity by decreasing rate of mitosis in comparison to water. Methotrexate (0.1 mg/mL) was used as a standard andshows the highest antimitotic activity. Thus, the selected plant displayed significant antimitotic activity by showing good inhibition. Stigmasterol and Squalene have demonstrated remarkable binding affinity towards Bcl-2 inhibitor (2W3L). Apigenin, Squalene and Kaempferol have demonstrated remarkable binding affinity towards VEGFR-2 inhibitor (2OH4) respectively. The comprehensive analysis of both in vitro and in silico data shows that the bark of selected plant could be a potent source of drug and could serve as an effective therapeutic in the future
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Haider, Kashif, and Mohammad Shahar Yar. "Advances of Benzimidazole Derivatives as Anticancer Agents: Bench to Bedside." In Benzimidazole [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.101702.

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Benzimidazole is one of the privileged nitrogen-containing scaffolds known for its versatile diversified role in insecticides, pesticides, dyes, pigments and pharmaceuticals. Due to its electron-rich environment, structural features and binding potency of various therapeutic targets, benzimidazole derivatives exhibit a broad spectrum of biological activity that majorly includes antimicrobial, antifungal, analgesics, anti-diabetic and anticancer agents. Several benzimidazole scaffolds bearing drugs are clinically approved; they are used for various indications. For example, Bilastine, Lerisetron, Maribavir and Nocodazole are the most widely used benzimidazole-based marketed drugs available as an antihistamine, antiviral and antimitotic agent, respectively. Another example is the recently approved anticancer drug Binimetinib and Selumetinib, which are indicated for BRAF mutated melanoma and plexiform neurofibromas. Not only this, many benzimidazole-based anticancer drugs are in late phases of clinical development. Due to the vast therapeutic potential of benzimidazole scaffold in cancer research, medicinal chemists have gained a lot of attraction to explore it more and develop novel, highly effective and target-specific benzimidazole-based potential anticancer drugs.
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Podila, Naresh, Sanapala Arun Kumar, Vijaya Kishore K., et al. "In-silico and In-vitro Antimitotic Activity of Some Novel 6-Fluoro-1, 2, 4-Triazolo-Benzothiazole Analogues." In Advanced Concepts in Pharmaceutical Research Vol. 5. B P International, 2024. http://dx.doi.org/10.9734/bpi/acpr/v5/7097e.

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Taber, Douglass F. "Alkaloid Synthesis: (−)-α-Kainic Acid (Ohshima), Serpentine (Scheidt), (−)-Galanthamine ( Jia), (+)-Trigolutes B (Gong), Sarain A (Yokoshima/Fukuyama), DZ-2384 (Harran)." In Organic Synthesis. Oxford University Press, 2017. http://dx.doi.org/10.1093/oso/9780190646165.003.0060.

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(−)-α-Kainic acid 3 is widely used in neuropharmacological studies. En route to 3, Takashi Ohshima of Kyushu University found (Chem. Eur. J. 2015, 21, 3937) that the intramolecular ene cyclization of 1 delivered 2 with high diastereocontrol. Karl A. Scheidt of Northwestern University set (Angew. Chem. Int. Ed. 2015, 54, 6900) the absolute configuration of 5 and so of serpentine 6 by the organocatalyzed cyclization of 4. This is the first total synthesis of that alkaloid. Yanxing Jia of Peking University prepared (Angew. Chem. Int. Ed. 2015, 54, 6255) the benzofuran 8 by the Pd-mediated cyclization of the alkyne 7. An organo­catalyzed intermolecular Michael addition set the absolute configuration of (−)-galanthamine 9. Liu-Zhu Gong of the University of Science and Technology of China assem­bled (Chem. Eur. J. 2015, 21, 8389) (+)-trigolutes B 13 by the organocatalyzed addition of 10 to 11 to give 12. Barry M. Trost of Stanford University employed (Chem. Sci. 2015, 6, 349) a similar strategy in a synthesis of (−)-perophoramidine (not illustrated). Satoshi Yokoshima and Tohru Fukuyama of Nagoya University showed (Angew. Chem. Int. Ed. 2015, 54, 7367) that on deprotection, 14 was converted to an eight-membered cyclic nitrone, that further cyclized to 15. This set the stage for the synthesis of sarain A 16. Patrick G. Harran of UCLA has extensively studied the complex alkaloid (−)-diazonamide A (not illustrated). Structural simplification and optimization of antimitotic activity led to the macrolactam DZ-2384 18. It is exciting that 18 could be prepared (Angew. Chem. Int. Ed. 2015, 54, 4818) on a multigram scale by selective electrochemical oxidation of the much simpler precursor 17.
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Conference papers on the topic "Antimitotic Activity"

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Burke, Patrick J., Joseph Z. Hamilton, Thomas A. Pires, Kim K. Emmerton, Peter D. Senter, and Scott C. Jeffrey. "Abstract A097: Tubulysin ADC payloads: An antimitotic drug class that retains activity in multidrug resistant models." In Abstracts: AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; October 26-30, 2019; Boston, MA. American Association for Cancer Research, 2019. http://dx.doi.org/10.1158/1535-7163.targ-19-a097.

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