Design, Synthesis, Molecular Docking and in vitro Evaluation of N-(4-Ethoxyphenylsulfonyl)pyrrolidine-2-carboxylic Acid Analogues as Antiangiogenic and Anticancer Agents on Multiple Myeloma

A. Ghosh, A. Saha, K. Sarker, S. Mishra and S. Sen*,

A.P.C. Ray Memorial Cancer Chemotherapeutic Research Unit, College of Pharmaceutical Sciences, Mohuda, Berhampur-760002, India

*Corresponding author: E-mail: prof.dr.subratasen@gmail.com

Abstract

In present work, N-(4-ethoxyphenylsulfonyl)pyrrolidine-2-carboxylic acid analogs were designed, synthesized and biologically evaluated as an antiangiogenic and anticancer agent on multiple myeloma. Compounds 3i, 3k and 3m exhibited the cytotoxic action on human multiple myeloma cell line RPMI8226 with IC50 (μM) value 3.72, 3.89 2.28, respectively. These compounds possessed the antiangiogenic property and are selectively cytotoxic to cancer cells, as observed from the in vitro study of human umbilical vein endothelial cell (HUVEC) and African green monkey epithelial cell (VERO), respectively. Antiproliferative assay of the compounds on HUVECs was carried out using the dye exclusion method with trypan blue. Molecular docking study of compound 3m with vascular endothelial growth factor receptor-2 (VEGFR-2) showed possible interaction with a binding energy -62.27 kcal/mol.

Keywords

Anti-angiogenesis, VEGFR-2, Multiple myeloma, Vero cell, N-(4-Ethoxyphenylsulfonyl)pyrrolidine-2-carboxylic acid.

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