Premium
Synthesis of Functionalized 1‐Aryl‐3‐phenylthiazolylpropanoids and Their Potential as Anticancer Agents
Author(s) -
Nana Frédéric,
Kuete Victor,
Zaharia Valentin,
Ngameni Bathelemy,
Sandjo Louis P.
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202002060
Subject(s) - cytotoxicity , thiazole , cytotoxic t cell , chemistry , combinatorial chemistry , cancer cell lines , aryl , anticancer drug , cancer cell , stereochemistry , drug , cancer , pharmacology , biochemistry , biology , in vitro , organic chemistry , alkyl , genetics
Natural products have inspired the development of multiple‐target anticancer agents. To reach this goal, preparation of hybrid molecules was adopted as a recent approach to target and affect both sensitive and resistant cells. In the continuation of the search for potent anticancer agents, nine thiazole‐based chalcones were prepared. Their cytotoxic activities were evaluated against twenty cancer cell lines and against the normal cell line AML12 hepatocytes. The key steps of these syntheses involved Hantzsch, Sommelet, and Claisen‐Schmidt reactions. Julia‐Colonna reaction was used to achieve the epoxidation of the double bond. The products were purified by chromatographic techniques and were characterized by spectroscopic methods. Cytotoxicity assays were performed by rezasurin reduction test. Compounds 4 – 10 showed promising cytotoxic activities. 4 and 7 were the most cytotoxic with IC 50 values lower than 1 μ M against seven and two cancer cell lines, respectively. This study disclosed a new series of potential anticancer agents among which 4 and 7 deserve further investigation to develop drug for sensitive and multidrug resistant (MDR) cancer.