Design, synthesis, and evaluation of novel combretastatin A‐4 based chalcone derivatives as anticancer agents
Bethi Rathnakar, Gajula Shyam Kumar, Saleem P. Mahammad, Gattu Sridhar, Sambaru Kalyani, Nimma Rameshwar, Mavurapu Satyanarayana
Abstract
Abstract 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.