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Design, Synthesis, and Cytotoxicity Evaluation of 3‐(5‐(3‐(aryl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐1‐phenyl‐4,5‐dihydro‐1H‐pyrazol‐3‐yl)pyridine and 5‐(3‐(aryl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐3‐(pyridin‐3‐yl)‐4,5‐dihydropyrazole‐1‐carbaldehyde Derivatives as Potential Anticancer Agents
Author(s) -
Alam Raquib,
Alam Md. Aftab,
Panda Amulya K.
Publication year - 2017
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2768
Subject(s) - cytotoxicity , hela , chemistry , aryl , cell culture , stereochemistry , cytotoxic t cell , pyridine , etoposide , in vitro , biochemistry , medicinal chemistry , organic chemistry , chemotherapy , medicine , alkyl , biology , genetics
In an attempt to find bio‐active small molecules, a series of novel 3‐(5‐(3‐(aryl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐1‐phenyl‐4,5‐dihydro‐1H‐pyrazol‐3‐yl)pyridine 5a–i and 5‐(3‐(aryl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐3‐(pyridin‐3‐yl)‐4,5‐dihydropyrazole‐1‐carbaldehyde 6a–i were designed, synthesized, and evaluated for their in vitro cytotoxic activity against a panel of human cancer cell lines namely; HeLa (human cervix), NCI‐H460 (human lung), PC‐3 (human prostate), and NIH‐3T3 (mouse embryo fibroblasts) normal cell line. Most of these compounds exhibited moderate to good cytotoxic activity against the tested cancer cell lines and weak toxicity against normal cell line. Analogues 5b , 5f , 5g , 6b, and 6g showed significant cytotoxicity as compared to standard drug etoposide. Among all the synthesized compounds, compound 6g displayed superior cytotoxicity with an IC 50 value of 7.98 ± 1.08 μM for Hela cancer cell line.