title: Synthesis of combretastatin A4 analogues on steroidal framework and their anti-breast cancer activity.
abstract: 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".
authors: Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Kukrail Picnic Spot Road, Lucknow 226015, U.P., India.
authors: Swati
authors: S
authors: Parihar
authors: Amit
authors: A
authors: Kumar
authors: Amit K
authors: AK
authors: Chaturvedi
authors: Naresh Kumar
authors: NK
authors: Sachan
authors: Suaib
authors: S
authors: Luqman
authors: Bendangla
authors: B
authors: Changkija
authors: Murli
authors: M
authors: Manohar
authors: Om
authors: O
authors: Prakash
authors: D
authors: D
authors: Chanda
authors: Feroz
authors: F
authors: Khan
authors: C S
authors: CS
authors: Chanotiya
authors: Karuna
authors: K
authors: Shanker
authors: Anila
authors: A
authors: Dwivedi
authors: Rituraj
authors: R
authors: Konwar
authors: Arvind S
authors: AS
authors: Negi
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000473:pathology*; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization; D013256:Steroids / Q000737:chemistry*; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013256:Steroids; D013267:Stilbenes; C058728:fosbretabulin
keywords: Acute oral toxicity; Antiestrogenicity; Breast cancer; Combretastatin A4; Estrogenicity; Tubulin polymerization inhibition