Design and Synthesis of Novel 2-Substituted-Benzyl-5-(2-Methylbenzofuran-3-Yl)-2H-Tetrazoles: Anti-Proliferative Activity

Sudhakar Mokenapelli^a, Madhu Gutam^a, Jayaprakash Rao Yerrabelli^a, Vamshi Krishna Irlapati^b, Neelima Gorityala^b, Someswar Rao Sagurthi^b and Prasad Rao Chitneni^{a, 1}

¹Phone: +91-9550506096; e-mail: prasadraoou@yahoo.com

^aNatural Products Laboratory, Department of Chemistry, Osmania University, Hyderabad-500007, Telangana, India;
^bDepartment of Genetics and Biotechnology, Osmania University, Hyderabad-500007, Telangana, India

Received 14.02.2020; revised 01.04.2020; accepted 06.04.2020

DOI: 10.1134/S1068162020050179

Abstract––A new series of 2,5-regioselective benzofuran-tetrazole hybrids (XIIIa–XIIIp) were synthesised from 2H-chromene-3-carbonitriles (IXa), (IXb) in multi steps approach under mild reaction conditions in good yields and evaluated their anti-proliferative activity against HCT116 and Miapaca2 cell lines. Wherein compounds (XIIIe) (IC₅₀: 3.19 μM) and (XIIIm) (IC₅₀: 2.25 μM) were displayed highest anti-proliferative activity in both cell lines. Molecular docking and SAR studies revealed the in vitro results with target Proto-oncogene tyrosine kinase Src protein.

Keywords: benzofuran, tetrazoles, anti-proliferative activity, molecular docking, SAR studies
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Полный текст статьи печатается в переводной версии журнала Russian Journal of Bioorganic Chemistry, V.46, Issue 5, P. 845–855 (Springer).