Synthesis and anticancer activity of oxindole derived imidazo[1,5-a]pyrazines
Synthesis and anticancer activity of oxindole derived imidazo[1,5-a]pyrazines
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DOI：
10.1016/j.ejmech.2011.03.027
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发表时间：
2011-06-01
影响因子：
6.7
通讯作者：
Ramakrishna, Sistla
中科院分区：
文献类型：
--
作者：
Kamal, Ahmed;Ramakrishna, G.;Ramakrishna, Sistla
A series of oxindole derivatives of imidazo[1,5-a]pyrazines were prepared and confirmed by (1)H NMR, mass and HRMS data. These compounds were evaluated for their anticancer activity against a panel of 52 human tumor cell lines derived from nine different cancer types: leukemia, lung, colon. CNS, melanoma, ovarian, renal, prostate and breast. Among them compound 71 showed significant anticancer activity with GI(50) values ranging from 1.54 to 13.0 mu M. Cell cycle arrest was observed in G0/G1 phase upon treatment of A549 cells with 6.5 mu M (IC(50)) concentration of compound 71 and induced apoptosis. This was confirmed by Annexin V-FITC as well as DNA fragmentation analysis and interestingly this compound (71) did not affect the normal cells. (C) 2011 Elsevier Masson SAS. All rights reserved.
