Novel 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-one derivatives as potential anti-cancer agents

Title
Novel 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-one derivatives as potential anti-cancer agents
Authors
Vani Nelamane Devegowda김정현한기철양은경추현아배애님남길수최경일
Keywords
6-N-Arylcarboxamidopyrazolo[4,3-d]-pyrimidin-7-one; Anticancer activity; Structure-activity relationship
Issue Date
2010-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, 1630-1633
Abstract
A novel series of 3,5,6-trisubstituted pyrazolo[4,3-d]pyrimidin-7-one derivatives, especially 6-N-arylcarboxamidopyrazolo[ 4,3-d]pyrimidin-7-ones were synthesized and evaluated for their in vitro anticancer activities against various human cancer cell lines. The inhibitory activities for several kinases have also been tested. The prepared compounds library exhibited significant anticancer activity towards HT-29 colon and DU-145 prostate cancer cell lines. The structure–activity relationships of the 6-N-arylcarboxamidopyrazolo[ 4,3-d]pyrimidin-7-one scaffold at R1, R2 and R3 have been elucidated. Among the synthesized compounds, 12b was the most active compound with GI50 value of 0.44 μMand 1.07 μM against HT-29 and DU-145 cell lines, respectively, and 13a was the most selective compound towards colon cancer cell line.
URI
http://pubs.kist.re.kr/handle/201004/37987
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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