Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents.

Sraa Abu-Melha,Sobhi Gomha,Nabila Kheder,Heba Salem,Mastoura Edrees,Mohamad Abdelaziz

doi:10.3390/molecules24030539

Abstract

A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, 11c and 6g, being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl4-induced hepatotoxicity.

Highlights

Synthesis of novel bioactive compounds using green methods that minimize the use and generation of hazardous substances, is a major aim for many researchers
[20,21,22,23,24,25], we present in this report an efficient synthesis of some new series approaches for the synthesis of different heterocyclic systems with auspicious pharmacological of novel [20,21,22,23,24,25], thiazolewederivatives using chitosan-grafted-poly(vinyl pyridine) as of annovel eco-friendly activities present in this report an efficient synthesis of some new series thiazole biopolymeric basic catalyst
We have efficiently synthesized a new series of thiazolylpyrazoles using hydrazonoyl halides and 2-cyano-N 0 -(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)acetohydrazide in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst

Summary

Introduction

Synthesis of novel bioactive compounds using green methods that minimize the use and generation of hazardous substances, is a major aim for many researchers. Many thiazole-containing drugs such as Abafungin, Alagebrium, Acotiamide, Amiphenazole, Brecanavir, Cefepime, Carumonam, and Cefmatilen are commercially available. Molecules 2019, 24, x FOR PEER REVIEW hepatoprotective activities [1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16]. Many thiazole-containing drugs such as Abafungin, Alagebrium, Acotiamide, Amiphenazole, Brecanavir, Cefepime, Carumonam, and Cefmatilen are Molecules 2019, 24, 539 commercially available. Cancer is regarded as one of the dominant causes of mortality nowadays. The development of new Cancer antitumor agents as represents urgent need to the increasing of various, is regarded one of theandominant causesdue of mortality nowadays.problems

Methods

Results

Conclusion