A REVIEW ON DOCKING STUDIES OF INDOLE MOIETY AS POTENT INHIBITOR OF TUBULIN POLYMERIZATION

Aditya Dixit; Devender Pathak; Gyanendra Kumar Sharma

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A REVIEW ON DOCKING STUDIES OF INDOLE MOIETY AS POTENT INHIBITOR OF TUBULIN POLYMERIZATION

机译：吲哚部分作为微管蛋白聚合潜在抑制剂的对接研究综述

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Aromatic heterocycles especially indole plays an important part in treatment of cancer. This review highlights compounds in development bearing indole moiety in their scaffold for the treatment of cancers. This review also highlights the utilization of colchicine binding site in order to inhibit tubulin polymerization. Docking studies shows that colchicine binding site is used by various indole derivatives to exert their action. Vincristine and vinblastine are the natural compounds which have the anticancer activity but they act on the vinca domain of the tubulin protein. Vinca domain can be too large for small ligands, so small molecules can utilize colchicines binding site to inhibit microtubule polymerization.

机译：芳香杂环，尤其是吲哚在癌症的治疗中起着重要的作用。这篇综述重点介绍了正在发展中的化合物，其支架中带有吲哚部分，可用于治疗癌症。这篇综述还强调了秋水仙碱结合位点的利用，以抑制微管蛋白的聚合。对接研究表明秋水仙碱结合位点被各种吲哚衍生物用来发挥其作用。长春新碱和长春碱是具有抗癌活性的天然化合物，但它们作用于微管蛋白的长春花碱域。长春花结构域对于小的配体而言可能太大，因此小分子可以利用秋水仙碱的结合位点来抑制微管聚合。

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《European Chemical Bulletin》 |2016年第11期|共5页
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Aditya Dixit; Devender Pathak; Gyanendra Kumar Sharma;
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3. Synthesis, Anticancer Activity and Molecular Modeling Studies of Novel Chalcone Derivatives Containing Indole and Naphthalene Moieties as Tubulin Polymerization Inhibitors [J] . Guangcheng Wang, Zhiyun Peng, Yongjun Li Chemical and Pharmaceutical Bulletin . 2019,第7期

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5. Preclinical evaluation and identification of potent tubulin and Hsp27 inhibitors as anticancer agents. [D] . Lama, Rati. 2015

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6. Synthesis biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives a new class of tubulin polymerization inhibitors [O] . Sultan Nacak Baytas, Nazan Inceler, Akın Yılmaz, -1

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7. Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors [O] . Sultan Nacak Baytas, Nazan Inceler, Akın Yılmaz, 2014

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8. Chemotherapeutic Potential of G1 Cell Cycle Inhibitor Indole-3-Carbinol and Its More Potent N-Alkoxy Derivatives in Human Breast Cancer Xenografts in Mice [R] . Kerekatte, V. S. , Firestone, G. 2004

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A REVIEW ON DOCKING STUDIES OF INDOLE MOIETY AS POTENT INHIBITOR OF TUBULIN POLYMERIZATION

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