Synthesis of novel 尾-carboline based chalcones with high cytotoxic activity against breast cancer cells

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• 作者：Shikha S. Chauhan^a ; ^c ; Anup K. Singh^b ; Sanjeev Meena^b ; Minaxi Lohani^c ; Akhilesh Singh^b ; Rakesh K. Arya^b ; Srikanth H. Cheruvu^d ; Jayanta Sarkar^b ; Jiaur R. Gayen^d ; Dipak Datta^b ; Prem M.S. Chauhan^a ; ^{prem_chauhan_2000@yahoo.com" class="auth_mail} ; ^{premsc58@hotmail.com" class="auth_mail}
• 关键词：Anticancer ; 尾-Carboline ; Chalcone ; Cytotoxic
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 July 2014
• 年：2014
• 卷：24
• 期：13
• 页码：2820-2824
• 全文大小：787 K

文摘

A series of novel 尾-carboline based chalcones was synthesized and evaluated for their cytotoxic activity against a panel of human cancer cell lines. Among them we found that two of the compounds 7c and 7d, showed marked anti-proliferative activity in a panel of solid tumor cell lines with highest effect in breast cancer. The compounds 7c and 7d showed an IC₅₀ of 2.25 and 3.29 渭M, respectively against human breast cancer MCF-7 cell line. Further, the compound 7c markedly induced DNA fragmentation and apoptosis in breast cancer cells.