Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 22, Pages 6781-6784Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.133
Keywords
Amidines; Pyrazoles; Antiproliferative activity; Microwave-assisted reaction; Formylation
Categories
Funding
- China Medical University [CMU98-NCTUS-08]
- National Science Council of Republic of China [NSC 99-2320-B-039-014-MY3]
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A series of N,N-disubstituted-N'-[1-aryl-1H-pyrazol-5-yl]-methnimidamides was synthesized by a newly developed microwave reaction and their antiproliferative activities were evaluated. Microwave irradiation of 5-amino-1,3-disubstituted pyrazoles with various amide solvents in the presence of POCl(3) provided the corresponding 2a-2k, 3a-3c, and 4a-4f in good to excellent yields. The obtained methnimidamides were tested against NCI-H661, NPC-TW01, and Jurkat cancer cell lines and the results indicated that compounds 2d and 2e were the most potent with IC(50) values in low micromolar range. (C) 2010 Elsevier Ltd. All rights reserved.
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