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Mini-Reviews in Medicinal Chemistry

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ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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Research Article

Synthesis, Antimicrobial and Antitumor Evaluations of a New Class of Thiazoles Substituted on the Chromene Scaffold

Author(s): Dina H. Elnaggar, Naglaa A. Abdel Hafez, Huda R.M. Rashdan, Nayera A.M. Abdelwahed, Hanem M. Awad and Korany A. Ali*

Volume 19, Issue 20, 2019

Page: [1717 - 1725] Pages: 9

DOI: 10.2174/1389557519666190722123422

Price: $65

Abstract

Background & Objective: A new series of thiazoles substituted on the chromene scaffold were prepared by facial approaches starting from (E)-1-(2,3-Dihydrochromen-4-ylidene)thiosemicarbazide derivatives (2a,b). The thiosemicarbazides (2a,b) were reacted with a series of α-halo carbonyl compounds to give the corresponding rhodanine analogues and reacted also with C-acetyl-or Cethoxy- N-hydrazonoyl chlorides to afford the corresponding tri- and tetra-substituted hybrid hydrazinyl thiazole substituted chromenes.

Methods: The newly synthesized compounds were screened for their in vitro antimicrobial and antitumor activities by agar diffusion method and MTT assay, respectively.

Results: The results of the antimicrobial activity revealed that some of the new compounds exhibited excellent activity against pathogenic microorganism; Candida albicans compared with Ciprofloxacin and nystatin, as the reference drugs.

All of the tested compounds exhibited significant cytotoxic activities comparable to that of the reference drug; Doxorubicin® (on HCT116 (colorectal carcinoma human cell line).

Keywords: Thiosemicarbazide, chromene scaffold, hydrazonoyl chlorides, antimicrobial activity, HCT116 (colorectal carcinoma), MTT assay.

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