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One-pot synthesis and antiproliferative evaluation of pyrazolo[3,4-d]pyrimidine derivatives |
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| Authors: | Yu-Ying HuangLi-Ya Wang Chun-Hsi ChangYueh-Hsiung Kuo Kimiyoshi KanekoHiroyuki Takayama Masayuki KimuraShin-Hun Juang Fung Fuh Wong |
| Affiliation: | a Graduate Institute of Pharmaceutical Chemistry, China Medical University, No. 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC b The Ph.D. Program for Cancer Biology and Drug Discovery, China Medical University, No. 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC c The Graduate Institute of Chinese Pharmaceutical Sciences, China Medical University, No. 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC d Tsuzuki Institute for Traditional Medicine, China Medical University, No. 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC e Department of Medico Pharmaceutical Science, Nihon Pharmaceutical University, 10281, Komuro, Inamachi, Kita-Adachigun, Saitama, Japan |
| Abstract: | An efficient one-pot methodology for the synthesis of pyrazolo[3,4-d]pyrimidines was developed by using 5-aminopyrazoles with formamide in presence of PBr3 as the coupling agent. Among the examples presented in this work, compounds 41 and 54-56 with phenyl or 2-quinolinyl groups at N-1 and p-Me-Ph, p-Cl-Ph, or p-OMe-Ph group at C-3 position in the pyrazole ring possessed better potency against NCI-H226 and NPC-TW01 cancer cells with GI50 values between 18 μM and 39 μM. |
| Keywords: | Pyrazolo[3,4-d]pyrimidines 5-Aminopyrazoles Antiproliferative activity One-pot synthesis |
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