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

页码：2321 / 2327

页数：7

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