Novel benzothiazine-piperazine derivatives by peptide-coupling as potential anti-proliferative agents

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• 作者：Ramineni Venkatesh^a ; Suresh Kasaboina^a ; Deepthi Bidayat^a ; U Nikhil Kumar^a ; Nishant Jain^b ; Saritha Jostna Tangeda^d ; Rajashaker Bantu^a ; Sridhara Janardhan^c ; ; Lingaiah Nagarapu^a ; ^{lnagarapuiict@yahoo.com} ; ^{nagarapu@iict.res.in}
• 关键词：Peptide-coupling ; Anti-proliferative activity ; Molecular docking ; Benzothiazine-piperazine ; HDAC8 ; EHMT2
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：354-359
• 全文大小：1159 K
• 卷排序：27

文摘

A new templates of benzothiazine-piperazine derivatives 8a–i and 10a–g were efficiently synthesized. Compound 10e obviously suppressed cancer cell proliferation and migration. Compounds 8g, 10f shown GI50 values <0.01 μM against IMR32, MDA-MB-231 cell lines. Compound 10e was well docked in HDAC8 and EHMT2 proteins.