Design and Synthesis of Glycoside Inhibitors of Glioma and Melanoma Growth

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• 作者：Isabel Garcí ; a-&Aacute ; lvarez ; Guillermo Corrales ; Ernesto Doncel-Pé ; rez ; Ana Muñ ; oz ; Manuel Nieto-Sampedro ; Alfonso Fern&aacute ; ndez-Mayoralas
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：January 25, 2007
• 年：2007
• 卷：50
• 期：2
• 页码：364 - 373
• 全文大小：169K
• 年卷期：v.50,no.2(January 25, 2007)
• ISSN：1520-4804

文摘

An N-acetylglucosaminide derivative with a pentaerythritol substituent at position C-6 was previouslysynthesized and shown to inhibit neural tumor growth. Now, we report the preparation of a series of newsynthetic compounds introducing systematic changes in the nature, polarity, and size of the sugar substituents.The antimitotic activity of the new compounds was tested on cultured rat (C6) and human (U-373) gliomalines and on a human melanoma line (A-375). The antimitotic and antitumoral activity of the new compoundson glioma cell lines increased up to 2 orders of magnitude with respect to the parent compound or wasabolished, permitting a detailed structure-function analysis of the new antitumorals. One of the glycosidesinhibited melanoma division with an ID₅₀ below the micromolar range.