My Blog

NEW THIAZOLONE DERIVATIVES: DESIGN, SYNTHESIS, ANTICANCER AND ANTIMICROBIAL ACTIVITY

NEW THIAZOLONE DERIVATIVES: DESIGN, SYNTHESIS, ANTICANCER AND ANTIMICROBIAL ACTIVITY

Author: Dattatraya N. Pansare, Rohini N. Shelke, Mininath C. Khade, Vrushali N. Jadhav, Chandraknat D. Pawar, Rajiv A. Jadhav, Saroj R. Bembalkar Silaev
Abstract

In order to explore the anticancer and antimicrobial activity associated with the thiazolone framework, several new (Z)-2-((5-(3-
fluorobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)carboxylic acid derivatives have been synthesized in water as a solvent. All
synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Amongst these, the 3-methylbutanoic and the 3- or 4-methylpentanoic acid derivatives, the 3-hydroxy-, the 3-(1H-imidazol-4-yl) and the 3-(4-hydroxyphenyl)propanoic acid derivatives and the succinic acid derivative showed high antibacterial and antifungal activity. The unsubstituted propanoic acid derivative exhibited significant antibacterial activity against B. subtilis and significant antifungal activity against fungal strains, i.e., A. flavus. The in vitro anticancer studies revealed that the 3-(hydroxy)-, the 3-(1H-imidazol-4yl)- and the 3-(4-hydroxyphenyl)propanoic acid, or the succinic acid derivatives are the most active compounds against MCF-7 and BT-474 human breast cancer cell lines.

Keywords: 2-thioxothiazolidin-4-one, 3-fluorobenzaldehyde, amino acids, anticancer, antimicrobial

Leave a Comment

Your email address will not be published. Required fields are marked *