Design, synthesis and biological evaluation of novel benzodioxole derivatives as COX inhibitors and cytotoxic agents.

ABSTRACT: Non-steroidal anti-inflammatory drugs are among the most used drugs. They are competitive inhibitors of cyclooxygenase (COX). Twelve novel compounds (aryl acetate and aryl acetic acid groups) were synthesized in this work in order to identify which one was the most potent and which group was most selective towards COX1 and COX2 by using an in vitro COX inhibition assay kit. The cytotoxicity was evaluated for these compounds utilizing MTS assay against cervical carcinoma cells line (HeLa). The synthesized compounds were identified using FTIR, HRMS, ¹H-NMR, and ¹³C-NMR techniques. The results showed that the most potent compound against the COX1 enzyme was 4f with IC₅₀ = 0.725 µM. The compound 3b showed potent activity against both COX1 and COX2 with IC₅

SUBMITTER: Hawash M 

PROVIDER: S-EPMC7487730 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature