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1‐Acetyl‐3,5‐diaryl‐4,5‐dihydro(1 H )pyrazoles: Exhibiting Anticancer Activity through Intracellular ROS Scavenging and the Mitochondria‐Dependent Death Pathway
Author(s) -
Alex Jimi M.,
Singh Sandeep,
Kumar Raj
Publication year - 2014
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201400199
Subject(s) - intracellular , apoptosis , mitochondrion , reactive oxygen species , programmed cell death , chemistry , cell culture , stereochemistry , cancer cell lines , structure–activity relationship , cell growth , cancer cell , pharmacology , cancer , biochemistry , biology , in vitro , genetics
A series of 17 analogs of 1‐acetyl‐4,5‐dihydro(1 H )pyrazoles ( JP‐1 to JP‐17 ) bearing two aromatic rings at positions 3 and 5, either of which ought to be heterocyclic, were synthesized and evaluated for their anti‐proliferative potential against breast cancer (MCF‐7 and T‐47D) and lung cancer (H‐460 and A‐549) cell lines for the first time. JP‐1 – 7 , ‐ 10 , ‐ 11 , ‐ 14 , and ‐ 15 were observed to exhibit significant anti‐proliferative activity against MCF‐7 cells. Some notions about structure–activity relationships are reported. The investigated compounds were found to lower the intracellular reactive oxygen species in the H 2 DCFDA assay and also caused mitochondria‐dependent cell death in the MCF‐7 cell line, indicating a plausible mechanism of their anticancer effect.