Synthesis and Evaluation of 5-Aryl-3-(4-hydroxyphenyl)-1,3,4-oxadiazole-2-(3H)-thiones as P-Glycoprotein Inhibitors

Chatchanok Loetchutinat; François Chau; Samlee Mankhetkorn

doi:10.1248/cpb.51.728

Notes

Synthesis and Evaluation of 5-Aryl-3-(4-hydroxyphenyl)-1,3,4-oxadiazole-2-(3H)-thiones as P-Glycoprotein Inhibitors

Chatchanok Loetchutinat, François Chau, Samlee Mankhetkorn

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Keywords: oxadiazolethione, multidrug resistance (MDR), P-glycoprotein, inhibitor

JOURNAL FREE ACCESS

2003 Volume 51 Issue 6 Pages 728-730

DOI https://doi.org/10.1248/cpb.51.728

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Abstract

5-Aryl-3-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 3 were prepared by cyclocondensation of 1-(4-hydroxyphenyl)-2-aroylhydrazines with thiophosgene. All compounds exhibited antiproliferation activity in K562, IC₅₀ ranging from 24 to 94 μM comparable efficacy with apigenin and genistein and showed more potent antiproliferation of K562/adr cells, highly expressing P-glycoprotein. Compounds 3g, 3e and 3a inhibited the function of P-glycoprotein with the α_0.5 equal to 10±3 μM, 21±5 μM and 34±7 μM, respectively.

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