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Design, synthesis, and evaluation of novel combretastatin A‐4 based chalcone derivatives as anticancer agents
Author(s) -
Rathnakar Bethi,
Kumar Gajula S.,
Mahammad Saleem P.,
Gattu Sridhar,
Kalyani Sambaru,
Nimma Rameshwar,
Satyanarayana Mavurapu
Publication year - 2021
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.4186
Subject(s) - chemistry , chalcone , combretastatin , stereochemistry , a549 cell , cell culture , cell growth , derivative (finance) , combinatorial chemistry , in vitro , biochemistry , microtubule , genetics , tubulin , economics , financial economics , biology , microbiology and biotechnology
A series of combretastatin A‐4 based chalcones ( 14a‐l ) were designed, synthesized and these compounds examined for inhibitory effects on the proliferation of human lung (A549), breast (MCF‐7), melanoma (A375), and colon (HT‐29) carcinoma cells. Compounds 14b , 14c , 14e , 14h , and 14i (tri/dimethoxy, methyl, and mono/dinitro derivatives) have exhibited the most potent antiproliferative activity with IC 50  < 2 μM and the hexa methoxy derivative 14b , the most promising one, which displayed the potent inhibitory activities in MCF‐7 (IC 50 : 10 nM), A375 (IC 50 : 12 nM), and A549 (IC 50 : 65 nM) cell lines, and is 18 times more potent than the CA‐4. Compound 14b represents a new scaffold and the results provide insights into further development of anticancer agents.

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