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Microwave-assisted synthesis of some novel fluorinated pyrazolo[3,4-d]pyrimidine derivatives containing 1,3,4-thiadiazole as potential antitumor agents
โ Scribed by Xin Jian Song; Yu Shao; Xing Gao Dong
- Publisher
- Chinese Electronic Periodical Services
- Year
- 2011
- Tongue
- English
- Weight
- 121 KB
- Volume
- 22
- Category
- Article
- ISSN
- 1001-8417
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โฆ Synopsis
A facile microwave-assisted procedure for synthesis of novel fluorinated pyrazolo [3,4-d]pyrimidine derivatives containing 1,3,4-thiadiazole is described. This protocol presented such advantages as short reaction time, high yields, simple purification and environmentally benign procedures. Their antitumor activities were evaluated against HL-60 by an MTT assay. The preliminary results indicated that some title compounds exhibit more potent antitumor inhibitory activity than doxorubicin (DOX).
๐ SIMILAR VOLUMES
## Abstract Compound (Ic) shows the most potent biological activity against HEPG2 cancer cell line, which is comparable to the positive control.
A series of triazines have been synthesized starting from 5-alkyl-1,3,4-thiadiazole-2-thioles (1a-d). On reaction with ethyl bromoacetate in the presence of anhydrous K 2 CO 3 under microwave irradiation (MWI), these yielded corresponding esters (2a-d) which on hydrazinolysis under MWI produced (5-a