Synthesis, Crystal Structure, and Antiproliferative Activity of Novel 7-Arylaminopyrazolo[1,5-a]pyrimidine Derivatives Containing the Hydrazone Moiety

被引：2
|
作者：
Shi, Jian-tao [1 ]
Chen, Ye [1 ]
Ji, Shengjun [2 ]
Ding, Shi [1 ]
Liu, Ju [1 ]
机构：
[1] Liaoning Univ, Coll Pharm, Key Lab New Drug Res & Dev Liaoning Prov, Shenyang 110036, Liaoning, Peoples R China
[2] Jilin Yimintang Pharmaceut Co LTD, Siping 136000, Jilin, Peoples R China
来源：
RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2019年 / 89卷 / 11期
关键词：
pyrazolo[1,5-a]pyrimidine; synthesis; X-ray diffraction; antiproliferation activity; BIOLOGICAL-ACTIVITY; DESIGN; POTENT;
D O I：
10.1134/S1070363219110252
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of novel 7-arylaminopyrazolo[1,5-a]pyrimidine derivatives containing the hydrazone moiety has been synthesized by a five-step procedure including cyclization, chlorination, amination, hydrazinolysis, and condensation. Structures of the products have been characterized by IR, H-1 NMR and MS spectra, and single-crystal X-ray diffraction. The bioassay results indicate most of the compounds as potentially antiproliferation agents against A549 and HT-29 cell lines. Among those, compounds 6e and 6f exhibit remarkable inhibitory activity against HT-29 cell lines, that are comparable with that of the positive control sorafenib. Preliminary structure-activity relationship is considered.
引用
收藏
页码：2321 / 2327
页数：7
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