Novel 2-(2-hydrazinyl)thiazole derivatives as chemotherapeutic agents

Abstract

A series of 2-(2-hydrazinyl)thiazole derivatives containing diarylsulfide moiety were synthesized and investigated for their antibacterial and antifungal activities. Compound 3j, namely 2-[2-[4-((4-fluorophenyl)thio)benzylidene]hydrazinyl]-4-(4-methylphenyl)thiazole was determined as the most potent antifungal agent. It was further tested to detect the apoptosis induction ratio on Candida spp. which is a new approach to identify the mechanism of action responsible for antifungal potency. Also, the inhibitory activity of all the target compounds against healthy cell line, NIH3T3, and tumor cell lines A549, Caco2, MCF-7, HL60, and K562 was determined by MTT assay. The activity results were found moderate and the first seven derivatives containing chloro substituent (3a–3g) exhibited more antiproliferative activity than those containing fluoro substituent.

Graphical Abstract

Keywords:

• 2-(2-Hydrazinyl)thiazole
• diarylsulfide
• antifungal
• antiproliferative
• apoptosis

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