New derivatives of 1,3,4-trisubstituted pyrazole have been synthesized via different reaction routs starting with the chalcone (E)-3-[3-(4-bromophenyl)-1-ethyl-1H-pyrazol-4-yl]-1-(4-chlorophenyl)prop-2-en-1-one and dicarbonitrile 2-[[3- (4-bromophenyl)-1-ethyl-1H-pyrazol-4-yl]methylene]malononitrile derived from 3-(4-bromophenyl)-1H-pyrazole-4-carb- aldehyde, and the in-vitro anti-cancer activity has been tested against various human cancer cell lines, namely: hepato- cellular carcinoma HepG2, breast cancer MCF7, lung carcinoma A549, prostatic cancer PC3, and colon carcinoma HCT116. Some of the tested analogs exhibited signiﬁcant activity on the target cell lines, and compound 4-[3-(4-bro- mophenyl)-1-ethyl-1H-pyrazol-4-yl]-1,2-dihydro-2-oxo-6-(pyridin-2-yl)pyridine-3-carbonitrile was not only the most potent among the tested compounds with IC = 9.130, 11.957, 9.130, 29.130, and 8.913 lM, compared with the reference standard doxorubicin (IC = 34.242, 20.851, 5.928, 38.024, 7.174 lM) on HepG2, MCF7, A549, PC3, and HCT116 cell lines, respectively, but also displayed no cytotoxic activity on the BJ-1 ﬁbroblast normal human cell line. Objectively, the newly synthesized analogs can serve as a brick for the development of potent anti-cancer agents. Graphical abstract IC 1.1 0.9 0.8 0.7 0.6 0.5 0.4 0.3 0.2 0.1 0 102030405060708090 100 Keywords Trisubstituted pyrazole Claisen–Schmidt Knoevenagel Anti-cancer Introduction Electronic supplementary material The online version of this article (https://doi.org/10.1007/s00706-018-2153-7) contains supplementary Cancer is a major worldwide health problem with material, which is available
Monatshefte für Chemie - Chemical Monthly – Springer Journals
Published: Feb 17, 2018
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