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Design, Synthesis, and Biological Evaluation of Pyrazole Derivatives
Author(s) -
Hu Chunqi,
Gao Yali,
Du Wenting
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12699
Subject(s) - pyrazole , hl60 , cell culture , chemistry , ic50 , in vitro , mdm2 , potency , biological activity , biochemistry , pharmacology , stereochemistry , biology , apoptosis , genetics
In this in vitro study , a series of novel pyrazole derivatives were designed, synthesized, and evaluated against five human cancer cell lines ( PC 3, A549, HL 60, HCT 116, and SW 620) for their antiproliferative and p53‐ MDM 2 binding inhibitory activities. Although biological evaluations showed that this series of compounds possessed weak p53‐ MDM 2 inhibitory activities, most of them displayed moderate to potent antiproliferative activities against the tested cells lines. Compound 11c exhibited the best potency for MDM 2 ( FP ‐ IC 50 = 29.22 μ m ) and demonstrated antiproliferative activities in response to the five tested cell lines ( IC 50 = 4.09–16.82 μ m ). Compared with the positive control Nutlin‐1, there was enhanced antiproliferative activity to p53‐mutated or p53‐deficient cell lines ( SW 620, HL 60, and PC 3).