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Title 

Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors

 

새로운 STAT3 저해제로 MD77의 생물학적 및 전산학적 평가

Authors 

D MasciocchiS VillaF MeneghettiA PedrettiD BarloccoL LegnaniL TomaByoung-Mog KwonS NakanoA AsaiA Gelain

Publisher 

Royal Society of Chemistry

Issue Date 

2012

Citation 

MedChemComm, vol. 3, no. 5, pp. 592-599

Abstract 

Signal Transducer and Activator of Transcription 3 (STAT3) is a latent cytoplasmic protein overexpressed in various cancer cell lines. STAT3 participates in oncogenesis by stimulating cell proliferation and preventing apoptosis and it has been proven as a suitable target for anticancer therapy. In order to identify direct STAT3 inhibitors, we performed a binding assay on several previously synthesized 1,2,5-oxadiazole derivatives. Among them, compound MD77, N-[4-(4-chlorophenyl)-1,2,5-oxadiazol-3-yl]-4-(trifluoromethyl) benzamide, showed a good ability to bind the STAT3-SH2 domain in a dose-dependent manner (IC 50 = 17.7 μM). Computational studies were carried out to investigate its binding mode. Moreover, compound MD77 showed a significant anti-proliferative activity versus several tumor cell lines. On these bases, compound MD77 was selected as a lead for the future development of direct STAT3 inhibitors.

ISSN 

2040-2503

Link 

http://dx.doi.org/10.1039/c2md20018j

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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