期刊
TETRAHEDRON
卷 68, 期 47, 页码 9658-9664出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.09.054
关键词
Pyrazolo[3,4-d]pyrimidines; 5-Aminopyrazoles; Antiproliferative activity; One-pot synthesis
资金
- China Medical University [CMU100-ASIA-17, CMU-101-S-23]
- Tsuzuki Institute for Traditional Medicine
- National Science Council of Republic of China [NSC-99-2320-B-039-014-MY3]
- Taiwan Department of Health Clinical Trial and Research Center of Excellence [DOH100-TD-B-111-004]
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 NCl-H226 and NPC-TW01 cancer cells with GI(50) values between 18 mu M and 39 mu M. (c) 2012 Elsevier Ltd. All rights reserved.
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