國家衛生研究院 NHRI:Item 3990099045/13875
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    題名: Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design
    作者: Yeh, TK;Song, JS;Chang, PW;Yu, JC;Chang, CH;Liao, FY;Tien, YW;Kuppusamy, R;Li, AS;Chen, CH;Chen, CW;Lin, LM;Chang, HH;Huang, CH;Yao, JY;Wu, MH;Peng, YH;Hsueh, CC;Hsiao, WC;Chen, PH;Lin, CY;Hsieh, SH;Shih, C;Hung, MS;Wu, SY;Kuo, CC;Ueng, SH
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Indoleamine 2,3-dioxygenase-1 (IDO1) is a potential target for the next generation of cancer immunotherapies. We describe the development of two series of IDO1 inhibitors incorporating a N-hydroxy-thiophene-carboximidamide core generated by knowledge-based drug design. Structural modifications to improve the cellular activity and pharmacokinetic (PK) properties of the compounds synthesized, including extension of the side chain of the N-hydroxythiophene-2-carboximidamide core, resulted in compound 27a, a potent IDO1 inhibitor which demonstrated significant (51%) in vivo target inhibition on IDO1 in a human SK-OV-3 ovarian xenograft tumor mouse model. This strategy is expected to be applicable to the discovery of additional IDO1 inhibitors for the treatment of other diseases susceptible to modulation of IDO1.
    日期: 2022-02-05
    關聯: European Journal of Medicinal Chemistry. 2022 Feb 5;229:Article number 114043.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2021.114043
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000766121600003
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85121273827
    顯示於類別:[翁紹華] 期刊論文
    [郭靜娟] 期刊論文
    [伍素瑩] 期刊論文
    [洪明秀] 期刊論文
    [石全(2014-2017)] 期刊論文
    [葉燈光] 期刊論文

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