Synthesis and Biological Evaluation of Dasatinib Amino Acid Derivatives as Potential Antitumor Agent

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：yjq360124

【摘要】

：

【作者】

：

Fei Liu LiWei Lang Ji Jiang HuaJun Lu JianMin Wang Shih-Chen Wang

【机构】

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Department of Nuclear Medicine,Peking Union Medical College & Chinese Academy of Medical Sciences,Pe

【出处】

：

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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　　Dasatinib was identified as potent orally administered Src/Abl kinase inhibitors with excellent antiproliferative activity against Philadelphia Chromosome-Positive Chronic Myelogenous Leukemia in chronic phase.The low bioavailability of Dasatinib may be due to both incomplete oral absorption and first-pass metabolism.A series of amino acid derivatives(Ⅰ) as potential prodrugs of Dasatinib were synthesized with the aim of improving aqueous solubility and therapeutic efficacy.The structures of these compounds were determined by IR,1H-NMR,13C-NMR and HRMS spectra.Preliminary in vivo studies indicated that some of derivatives had significantly improved oral bioavailability(~41%,rat) than of the reference drug(Dasatinib,14%),but the result need to get confirmed by further investigations.

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Synthesis and Biological Evaluation of Dasatinib Amino Acid Derivatives as Potential Antitumor Agent

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