Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors

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• 作者：Md Jawaid Akhtar^a ; Anees Ahmad Siddiqui^a ; Ahsan Ahmed Khan^a ; Zulphikar Ali^a ; Rikeshwer Prasad Dewangan^b ; Santosh Pasha^b ; M. Shahar Yar^a ; ^{yarmsy@rediffmail.com}
• 关键词：Benzimidazole linked oxadiazole ; Anticancer ; Apoptosis ; 3D-QSAR studies
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：853-869
• 全文大小：4705 K
• 卷排序：126

文摘

A series of twenty nine benzimidazole linked oxadizole were synthesized. All the compounds were screened for their anticancer and in vitro EGFR and erbB2 receptor inhibition assay. Two of the compounds 7a and 7n displayed promising activity. The compounds 7a showed EGFR inhibition; induce apoptosis; G2/M cell cycle arrest. Docking and QSAR studies of the compound 7a and 7n are reported.