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

Abstract：

: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 (1)H NMR, (13)C NMR and X-ray analysis.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Lesyk R,Vladzimirska O,Holota S,Zaprutko L,Gzella A

doi

10.1016/j.ejmech.2006.12.006

subject

Has Abstract

pub_date

2007-05-01 00:00:00

pages

641-8

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00004-9

journal_volume

42

pub_type

杂志文章

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