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Synthesis of new arylisoxazole–oxindole conjugates as potent antiproliferative agents
Author(s) -
Kumar Gajjela Bharath,
Bukhari Syed Nasir Abbas,
Qin HuaLi
Publication year - 2017
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.12884
Subject(s) - cytotoxicity , oxindole , hela , chemistry , stereochemistry , ic50 , conjugate , substituent , lung cancer , cell culture , combinatorial chemistry , pharmacology , cell , biochemistry , in vitro , biology , medicine , mathematics , mathematical analysis , catalysis , genetics
A new series of arylisoxazole–oxindole derivatives ( 6a–r ) were synthesized and evaluated for their antiproliferative activity against human cancer cell lines including non‐small cell lung (A549), cervical (HeLa), breast ( MCF ‐7), and prostate ( DU ‐145) cancer cell lines. The synthesized compounds ( 6a–r ) demonstrated excellent to moderate cytotoxicity with IC 50 values ranging from 0.82 to 3.69 μ m . Some new compounds ( 6m–r ) exhibited profound cytotoxicity better or similar to positive control. More particularly, the compound 6q possesses donating substituent like methoxy group presented at 5‐position on D ring exhibited remarkable antiproliferative activity against A‐549 (lung cancer) with an IC 50 value 0.82 μ m . Further studies to determine the mechanistic aspects of these conjugates are under progress.