Devegowda, Vani N. Kim, Jung Hyun Han, Ki-Cheol Yang, Eun Gyeong Choo, Hyunah Pae, Ae Nim Nam, Ghilsoo Choi, Kyung Il 2024-01-20T19:34:16Z 2024-01-20T19:34:16Z 2021-09-02 2010-03-01 0960-894X https://pubs.kist.re.kr/handle/201004/131645 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 R-1, R-2 and R-3 have been elucidated. Among the synthesized compounds, 12b was the most active compound with GI(50) value of 0.44 mu M and 1.07 mu M against HT-29 and DU-145 cell lines, respectively, and 13a was the most selective compound towards colon cancer cell line. (C) 2010 Published by Elsevier Ltd. English Pergamon Press Ltd. CANCER-RESEARCH INHIBITORS PHOSPHODIESTERASE-5 Novel 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-one derivatives as potential anti-cancer agents Article 10.1016/j.bmcl.2010.01.029 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.5, pp.1630 - 1633 Bioorganic & Medicinal Chemistry Letters 20 5 1630 1633 scie scopus 000274714600037 2-s2.0-76649107345 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CANCER-RESEARCH INHIBITORS PHOSPHODIESTERASE-5 6-N-Arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-one Anticancer activity Structure-activity relationship