Design and synthesis of imidazo[2,1-b]thiazole linked triazole conjugates: Microtubule-destabilizing agents

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• 作者：Siddiq Pasha Shaik^a ; ^b ; V. Lakshma Nayak^a ; Faria Sultana^a ; A.V. Subba Rao^a ; ^b ; Anver Basha Shaik^a ; Korrapati Suresh Babu^a ; Ahmed Kamal^a ; ^b ; ^c ; ^{ahmedkamal@iict.res.in}
• 关键词：Imidazo[2 ; 1-b]thiazoles ; Triazole conjugates ; Cytotoxicity ; Tubulin depolymerization ; Apoptosis
• 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：36-51
• 全文大小：3428 K
• 卷排序：126

文摘

Imidazo[2,1-b]thiazole linked triazole conjugates (4a–x) showed antiproliferative activity. Conjugates 4g and 4h arrested in G2/M Phase. Conjugates inhibit tubulin polymerization and disrupt microtubule organization. Western blot analysis revealed that Bax and Bcl-2 induced apoptosis.