New 5-substituted thiazolo[3,2-b][1,2,4]triazol-6-ones:: Synthesis and anticancer evaluation

被引：155

作者：

Lesyk, Roman ^{[1
]}

Vladzimirska, Ena

Holota, Serhiy

Zaprutko, Lucjusz

Gzella, Andrzej

机构：

[1] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, UA-79010 Lvov, Ukraine

[2] Poznan Univ Med Sci, Dept Organ Chem, PL-60780 Poznan, Poland

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 42卷 / 05期

关键词：

thiazolo[3,2-b][1,2,4]triazol-6-ones; X-ray study; anticancer activity;

D O I：

10.1016/j.ejmech.2006.12.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Following [2+3]-cyclocondensation reaction of 1,2,4-triazole-3(5)-thiol with N-arylmaleimides or with monochloroacetic acid and oxocompounds, N-(R-phenyl)-(6-oxo-5,6-dihydro[1,3]thiazol[3,2-b][1,2,4]triazol-5-yl)acetamides (1-5) and 5-ylidene-[1,3]thiazolo[3,2-b][1,2,4]triazol-6-ones (6-11) were synthesized as possible anticancer agents. Anticancer activity evaluation on the full panel of nearly 60 human cancer cell lines showed that synthesized compounds displayed this kind of activity on renal cancer, leukemia, colon cancer, breast cancer and melanoma cell lines. It was shown that 5-ylidene-[1,3]thiazolo[3,2-b][1,2,4]triazol-6-ones are characterized with more potent anticancer activity than respective amides. The structures of the compounds were determined by H-1 NMR, C-13 NMR and X-ray analysis. (c) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：641 / 648

页数：8

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