Synthesis and Evaluation of 5-Aryl-3-(4-hydroxyphenyl)-1,3,4-oxadiazole-2-(3H)-thiones as P-Glycoprotein Inhibitors
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概要
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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, IC_<50> ranging from 24 to 94μM 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±3μM, 21±5μM and 34±7μM, respectively.
- 公益社団法人日本薬学会の論文
- 2003-06-01
著者
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Mankhetkorn S
Laboratory Of Physical Chemistry Molecular And Cellular Biology Faculty Of Science Burapha Universit
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Mankhetkorn Samlee
Laboratory Of Physical Chemistry Molecular And Cellular Biology Faculty Of Science Burapha Universit
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LOETCHUTINAT Chatchanok
Laboratory of Physical Chemistry Molecular and Cellular Biology, Faculty of Science, Burapha Univers
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CHAU Francois
Laboratoire de Chimie organique medicale, Universite
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MANKHKTKORN Samlee
Laboratory of Physical Chemistry Molecular and Cellular Biology, Faculty of Science, Burapha Univers
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Loetchutinat Chatchanok
Laboratory Of Physical Chemistry Molecular And Cellular Biology Faculty Of Science Burapha Universit
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Mankhetkorn Samlee
Laboratory Of Physical Chemistry Molecular And Cellular Biology Department Of Radiologic Technology
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Chau Francois
Laboratoire De Chimie Organique Medicale Universite
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