Structure activity relationship of arylidene pyrrolo and pyrido [2,1-b] quinazolones as cytotoxic agents: Synthesis, SAR studies, biological evaluation and docking studies

Veenu Mangla, Kunal Nepali, Gagandip Singh, Jagjeet Singh, Santosh Guru, Manish Kumar Gupta, Priya Mahajan, Ajit Kumar Saxena, Kanaya Lal Dhar

研究成果: 雜誌貢獻文章同行評審

7 引文 斯高帕斯(Scopus)

摘要

Tubulin is the one of the most useful and strategic molecular targets for anticancer drugs. Agents that bind in Colchicine-binding site of tubulin include Phenstatin, Combretastatin A-4, Colchicine, Steganacin, Podophyllotoxin and certain other synthetic analogues of these compounds. Arylidene pyrollo and pyrido [2,1-b] quinazolones (isoindigatone and its synthetic analogues) have been earlier reported to be tubulin inhibitors evidenced by tubulin polymerization assay. The present study is an extension of the library of the isoindigatone and its synthetic analogues to generate the structure activity relationship. The study explores the role of the arylidene ring and also provides some intresting observations such as the placement of bicyclic ring such as naphylidene for potential activity. Some of the important interactions of KNH-3 and KNH-11 with the amino acid residues of active site of Tubulin have also been observed by molecular modeling.
原文英語
頁(從 - 到)642-650
頁數9
期刊Medicinal Chemistry
9
發行號5
DOIs
出版狀態已發佈 - 八月 1 2013
對外發佈

ASJC Scopus subject areas

  • 藥物發現

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