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Synthesis of Morpholine Linked Indole-1,2,3-triazole Hybrids as In Vitro Tubulin Polymerization Inhibiting Agents
Russian Journal of Bioorganic Chemistry ( IF 1 ) Pub Date : 2024-04-09 , DOI: 10.1134/s1068162024020018
Prasad Pinnoju , Sadanandam Kudikala , Manasa Scandakashi , Madavi Ramesh , Sarasija Madderla

Abstract

Objective: Synthesis of some new some new morpholine linked indole-1,2,3-triazole hybrids and evaluation of their anti-cancer activity. Methods: Cu (I) catalyzed azide-alkyne cycloaddition. MTT assay was used in anticancer activity. Autodock tools were used foe docking studies. Results and Discussion: All the sixteen compounds were screened against A549 (lung), MCF-7 (breast), and HeLa (cervical) and compared with nocodazole. In addition to this tubulin polymerization inhibition assay and docking studies were performed on some active compounds. Conclusions: Synthesized some new 1,2,3-triazole hybrids and screened them for anticancer activity, tubulin polymerization inhibition, and binding interaction with tubulin. Some of the compounds were found active.



中文翻译:

吗啉连接的吲哚-1,2,3-三唑杂化物作为体外微管蛋白聚合抑制剂的合成

摘要

目的:合成一些新的吗啉连接的吲哚-1,2,3-三唑杂化物并评价其抗癌活性。方法: Cu(I) 催化叠氮-炔环加成。 MTT法用于抗癌活性。 Autodock 工具用于对接研究。结果与讨论:所有 16 种化合物均针对 A549(肺)、MCF-7(乳腺癌)和 HeLa(宫颈)进行筛选,并与诺考达唑进行比较。除此之外,还对一些活性化合物进行了微管蛋白聚合抑制测定和对接研究。结论:合成了一些新的1,2,3-三唑杂化物,并筛选了它们的抗癌活性、微管蛋白聚合抑制以及与微管蛋白的结合相互作用。一些化合物被发现具有活性。

更新日期:2024-04-09
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