Synthesis of some new thiazole derivatives and their cytotoxicity on different human tumor cell lines


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Abstract

Some novel 1-(inden-3-ylidene)-2-(thiazol-2-ylidene)hydrazine derivatives 39 were synthesized by the Hantzsch reaction of thiosemicarbazone derivatives 2a2c with halo ketones and halo esters. Thiosemicarbazone derivatives reacted with hydrozonyl chlorides to give diazenyl-4-methylthiazole derivatives 11a11d. Structures of the products were elucidated from IR, 1H, and 13C NMR, and Mass spectra elucidate. The synthesized compounds were screened for their cytotoxicity against three human tumor cell lines. Twenty compounds showed high (≥60 %) antiproliferative activity over breast cancer (MCF-7). Compounds 2b, 3c, 4a, 4b, 6b, 6c, 7b, 8a, and 11b possessed higher cytotoxic activity over breast tumor cell line than Doxorubicin.

About the authors

A. M. Mohamed

Chemistry Department, College of Science; Applied Organic Chemistry Department

Author for correspondence.
Email: ammewas1@gmail.com
Saudi Arabia, Sakaka, Al-Jouf, 72341; Dokki, Cairo, 12622

N. A. Abdel-Hafez

Applied Organic Chemistry Department

Email: ammewas1@gmail.com
Egypt, Dokki, Cairo, 12622

A. F. Kassem

Department of Chemistry of Natural and Microbial Products

Email: ammewas1@gmail.com
Egypt, Dokki, Cairo

E. M. H. Abbas

Department of Chemistry of Natural and Microbial Products

Email: ammewas1@gmail.com
Egypt, Dokki, Cairo

M. M. Mounier

Pharmacognosy Department, Drug Bioassay-Cell Culture Laboratory, Pharmaceutical and Drug Industries Division

Email: ammewas1@gmail.com
Egypt, Dokki, Cairo


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