Synthesis and anticancer activity of N-9- and N-7- substituted 1,2,3 triazole analogues of 2,6-di-substituted purine

被引：0
|
作者：
Jabeena Khazir
Bilal Ahmad Mir
Gousia Chashoo
Lynne Pilcher
Darren Riley
机构：
[1] Government Degree College (Boys),Department of Chemistry
[2] University of Kashmir,Department of Botany, Satellite Campus Kargil
[3] CSIR-Indian Institute of Integrative Medicine,Cancer Pharmacology Division
[4] Canal Road,Department of Chemistry
[5] University of Pretoria,undefined
来源：
Medicinal Chemistry Research | 2020年 / 29卷
关键词：
2,6 Dichloropurine; Cycloaddition; 1,2,3 triazoles; anticancer;
D O I：
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摘要：
A library of N-9- and N-7-substituted 1,2,3 triazole analogues were generated on the 2,6-di-substituted purine upon reaction with various substituted aromatic azides. The synthesised analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like (HCT-1 (colon), THP-1 (leukaemia), IMR-32 (neuroblastoma) and A-549 (lung)). From the bioassay results, it was observed that even though most of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, but few of the analogues like 9a, 9b and 9e were found to be the most potent analogues in the series, with compound 9a showing IC50 values of 0.08 and 0.4 μM against THP-1 and A-549 cell lines, respectively.
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页码：33 / 45
页数：12
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