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Synthesis and antiproliferative activity of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles.

Abstract：

:A number of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles were synthesized and evaluated for their antiproliferative activities. The panel substitution included alkyl, aryl, and morpholinoalkyl derivatives. The structures of compounds were identified from elemental, IR, (1)H NMR, (13)C NMR and MS spectra analyses. The cytotoxicity in vitro against the four human cell lines: SW707 (rectal), HCV29T (bladder), A549 (lung), and T47D (breast) was determined. Alkyl and morpholinoalkyl derivatives exhibited significantly lower effect than phenyl ones. The highest antiproliferative activity was found for 2-(2,4-dichlorophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole, with ID(50) two times lower (SW707, T47D) than for cisplatin studied comparatively as the control compound.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Matysiak J,Opolski A

doi

10.1016/j.bmc.2006.02.027

subject

Has Abstract

pub_date

2006-07-01 00:00:00

pages

4483-9

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00179-9

journal_volume

14

pub_type

杂志文章

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