Synthesis of new arylisoxazole-oxindole conjugates as potent antiproliferative agents

被引:5
作者
Kumar, Gajjela Bharath [1 ]
Bukhari, Syed Nasir Abbas [1 ]
Qin, Hua-Li [1 ]
机构
[1] Wuhan Univ Technol, Sch Chem Chem Engn & Life Sci, Dept Pharmaceut Engn, Wuhan, Peoples R China
关键词
antiproliferative activity; arylisoxazole-oxindole; cancer; drug discovery; nocodazole; BIOLOGICAL EVALUATION; TUBULIN POLYMERIZATION; DESIGN;
D O I
10.1111/cbdd.12884
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 IC50 values ranging from 0.82 to 3.69 mu 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 IC50 value 0.82 mu m. Further studies to determine the mechanistic aspects of these conjugates are under progress.
引用
收藏
页码:634 / 638
页数:5
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