Synthesis and antiproliferative evaluation of N,N-disubstituted-N′-[1-aryl-1H-pyrazol-5-yl]-methnimidamides

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• 作者：Kaung-Min Cheng ; Yu-Ying Huang ; Jiann-Jyh Huang ; Kimiyoshi Kaneko ; Masayuki Kimura ; Hiroyuki Takayama ; Shin-Hun Juang ; Fung Fuh Wong
• 关键词：Amidines ; Pyrazoles ; Antiproliferative activity ; Microwave-assisted reaction ; Formylation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 November 2010
• 年：2010
• 卷：20
• 期：22
• 页码：6781-6784
• 全文大小：213 K

文摘

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 POCl₃ 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 IC₅₀ values in low micromolar range.