Synthesis and biological evaluation of novel 4,7-dihydroxycoumarin derivatives as anticancer agents |
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Authors: | Pilli Govindaiah Naresh Dumala Paramjit Grover M Jaya Prakash |
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Institution: | 1. Department of Chemistry, National Institute of Technology, Rourkela, Odisha 769008, India;2. Toxicology Unit, Applied Biology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, Telangana, India |
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Abstract: | A series of novel 4,7-dihydroxycoumarin based acryloylcyanohydrazone derivatives were synthesized and evaluated for antiproliferative activity against four different cancer cell lines (A549, HeLa, SKNSH, and MCF7). Most of the compounds displayed potent cytotoxicity with IC50 values ranging from 3.42 to 31.28 µM against all the tested cancer cell lines. The most active compound, 8h was evaluated for pharmacological mechanistic studies on cell cycle progression and tubulin polymerization inhibition assay. The results revealed that the compound 8h induced the cell cycle arrest at G2/M phase and inhibited tubulin polymerization with IC50 = 6.19 µM. Experimental data of the tubulin polymerization inhibition assay was validated by molecular docking technique and the results exhibited strong hydrogen bonding interactions with amino acids (ASN-101, TYR-224, ASN-228, LYS-254) of tubulin. |
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Keywords: | Corresponding author 4 7-Dihydoxycoumarin Acryloylcyanohydrazone Anticancer Cell cycle Tubulin Molecular docking |
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