The Synthesis of Tetrahydroquinazolone Derivatives for the Activation of Transcription Factor Nrf2 a

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户：bjkhs

【摘要】

：

【作者】

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Jau-Yang Chen Fong-Pin Liang Shin-Hun Juang Chih-Shiang Chang

【机构】

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Graduate Institute of Pharmaceutical Chemistry,College of Pharmacy,China Medical University,404 Taic

【出处】

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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会

【发表日期】

：

2012年8期

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　　Nuclear factor(erythroid-derived 2)-like 2(Nrf2) is a critical transcription factor regulating a cellular protective response that defends cells against toxic insults from a broad spectrum of chemicals.The activation of Nrf2 possesses chemopreventive activity against chemical carcinogenesis.A series of tetrahydroquinazolone derivatives was synthesized and bioevaluated for the Nrf2activity on the nasopharyngeal carcinoma TW01-9ARE-B3.The introduction of 3-pyridinylamino moiety onto 2-position of tetrahydroquinazolone possessed the 3-fold activation of Nrf2 in vitro study.

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The Synthesis of Tetrahydroquinazolone Derivatives for the Activation of Transcription Factor Nrf2 a

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