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

被引:33
作者
Parihar, Swati [1 ]
Kumar, Amit [2 ]
Chaturvedi, Amit K. [1 ]
Sachan, Naresh Kumar [1 ]
Luqman, Suaib [1 ]
Changkija, Bendangla [2 ]
Manohar, Murli [2 ]
Prakash, Om [1 ]
Chanda, D. [1 ]
Khan, Feroz [1 ]
Chanotiya, C. S. [1 ]
Shanker, Karuna [1 ]
Dwivedi, Anila [2 ]
Konwar, Rituraj [2 ]
Negi, Arvind S. [1 ]
机构
[1] CSIR, CIMAP, Lucknow 226015, UP, India
[2] CSIR, CDRI, Lucknow 22612, UP, India
关键词
Combretastatin A4; Breast cancer; Tubulin polymerization inhibition; Estrogenicity; Antiestrogenicity; Acute oral toxicity; RESVERATROL OLIGOMERS; LACTATE-DEHYDROGENASE; STILBENES; AGENTS; DERIVATIVES; INHIBITION; APOPTOSIS; BARK; CELL; PROLIFERATION;
D O I
10.1016/j.jsbmb.2013.02.009
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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". (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:332 / 344
页数:13
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