title: Synthesis and antiproliferative evaluation of N,N-disubstituted-N'-[1-aryl-1H-pyrazol-5-yl]-methnimidamides.
abstract: 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.
authors.affiliation: Graduate Institute of Pharmaceutical Chemistry, China Medical University, No. 91 Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC.
authors.forename: Kaung-Min
authors.initials: KM
authors.lastname: Cheng
authors.forename: Yu-Ying
authors.initials: YY
authors.lastname: Huang
authors.forename: Jiann-Jyh
authors.initials: JJ
authors.lastname: Huang
authors.forename: Kimiyoshi
authors.initials: K
authors.lastname: Kaneko
authors.forename: Masayuki
authors.initials: M
authors.lastname: Kimura
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Takayama
authors.forename: Shin-Hun
authors.initials: SH
authors.lastname: Juang
authors.forename: Fung Fuh
authors.initials: FF
authors.lastname: Wong
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D011720:Pyrazoles