Design, Synthesis and Antiproliferative Evaluation of N'-(1,3-Diaryl-lH-pyrazol-5-yl)-N,N-dimethylformamidine and N'-(4-Formyl-l,3-diaryl-lH-pyrazol-5-yl)-N,N-dimethylformamidine

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會 > Item 310902800/24194

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標題:	Design, Synthesis and Antiproliferative Evaluation of N'-(1,3-Diaryl-lH-pyrazol-5-yl)-N,N-dimethylformamidine and N'-(4-Formyl-l,3-diaryl-lH-pyrazol-5-yl)-N,N-dimethylformamidine
作者:	Yu-Ying Huang (黃俞穎) Kau-Shan Wen Kimiyoshi Kaneko Hiroyuki Takayama Masayuki Kimura Shin-Hun Juang Fung Fuh Wong (翁豐富)
日期:	2011
上傳時間:	2011-06-23 14:56:50 (UTC+8)
摘要:	Two classes of N'-(l,3-diaiy-1H--pyrazol-5-yl)-N,N-dimethylformamidine and N'-(4-formyl-l ,3-diaryl- 1H-pyrazol-5-yl)-N,N-dimethylformamidine were designed and synthesized by a chemoselective microwave-assisted amidination for evaluation of their difference of antiproliferative activities. A new chemoselective microwave irradiation of 5-amino-1,3 -disubstituted pyrazoles with N,N-methylformamide in the presence of POCl3 was successfully developed to alternatively synthesize presence of POCl3 was successfully developed to alternatively synthesize methnimidamides and pyrazolyl-2-azadienes two class compounds by using the tested against NCI-H226, NPC-TW01, and Jurkat cancer cell lines. Furthermore, the starting material 5-amino-l,3-disubstituted pyrazoles and de-amidination 5-amino-4-formyl-l,3-disubstituted pyrazoles were also used as the comparison molding cases for the structure activity relationship study. Following the SAR result, methnimidamide compounds 2b, 2c and 2d possessed the best potent with IC50 values in low micromolar range. On the other hand, We found the formyl group at C-4 position and the grafting amidinyl group in the pyrazolic main core molecule are necessary for the inhibitory activity.
關聯:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
顯示於類別:	[藥理學院] 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會

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