Synthesis of combretastatin A4 analogues on steroidal framework and their anti-breast cancer activity

详细信息    查看全文

• 作者：Swati Parihar ; Amit Kumar ; Amit K. Chaturvedi ; Naresh Kumar Sachan ; Suaib Luqman ; Bendangla Changkija ; Murli Manohar ; Om Prakash ; D. Ch ; a ; Feroz Khan ; C.S. Chanotiya ; Karuna Shanker ; Anila Dwivedi ; Rituraj Konwar ; Arvind S. Negi
• 关键词：Combretastatin A4 ; Breast cancer ; Tubulin polymerization inhibition ; Estrogenicity ; Antiestrogenicity ; Acute oral toxicity
• 刊名：The Journal of Steroid Biochemistry and Molecular Biology
• 出版年：2013
• 出版时间：September, 2013
• 年：2013
• 卷：137
• 期：Complete
• 页码：332-344
• 全文大小：1348 K

文摘

Combretastatin A4 analogues were synthesized on steroidal framework from gallic acid with a possibility of anti-breast cancer agents. Twenty two analogues were synthesized and evaluated for cytotoxicity against human breast cancer cell lines (MCF-7 & MDA-MB 231). The best analogue 22 showed potent antitubulin effect. Docking experiments also supported strong binding affinity of 22 to microtubule polymerase. In cell cycle analysis, 22 induced apoptosis in MCF-7 cells significantly. It was found to be non-toxic up to 300 mg/kg dose in Swiss albino mice in acute oral toxicity.

This article is part of a Special Issue entitled ¡°Synthesis and biological testing of steroid derivatives as inhibitors¡±.