W. Jin
2015
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0
Influential Citations
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Citations
Quality indicators
Journal
Chinese Journal of Synthetic Chemistry
Abstract
4-( 5-Chloro-3-methyl-1-phenyl-4-pyrazolyl)-3,4-dihydronpyrimidin-2( 1H)-( thio) one( 3) was prepared by Vilsmeier-Haack and Biginelli reaction using 3-methyl-1-phenyl-2-pyrazolin-5-one as the raw materials. Five novel thiazolo[3,2-a]pyrimidine derivatives containing pyrazole group( 5a ~ 5e) were synthesized by Knoevenagel reactions of 3 with arylaldehyde. The structures were characterized by1 H NMR,13 C NMR,IR and ESI-MS. The preliminary in vitro anticancer activities of 5a ~ 5e against human prostate cancer PC-3 cells were tested by MTT assay. The results showed that 5a ~ 5e exhibited certain anticancer activities and 2-【4-{ [6-( ethoxycarbonyl)-5-( 5-chloro-3-methyl-1-phenyl-4-pyrazolyl)-3-oxo-7-methyl-thiazolo [3,2-a]pyrimidin-2( 5H)-ylidene]methyl }phenoxy】acetic acid( 5a) exhibited the strongest anticancer activities with IC50 of 44. 45 μM.