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天然产物杂合体作为药物发现的新先导物。

Natural product hybrids as new leads for drug discovery.

作者信息

Tietze Lutz F, Bell Hubertus P, Chandrasekhar Srivari

机构信息

Institut für Organische Chemie, Georg-August-Universität Göttingen, Tammannstrasse 2, 37 077 Göttingen, Germany.

出版信息

Angew Chem Int Ed Engl. 2003 Sep 5;42(34):3996-4028. doi: 10.1002/anie.200200553.

Abstract

Natural products play an important role in the development of drugs, especially for the treatment of infections and cancer, as well as immunosuppressive compounds. However, the number of natural products is limited, whereas millions of hybrids as combinations of parts of different natural products can be prepared. This new approach seems to be very promising in the development of leads for both medicinal and agrochemical applications, as the biological activity of several new hybrids exceeds that of the parent compounds. The advantage of this concept over a combinatorial chemistry approach is the high diversity and the inherent biological activity of the hybrids.

摘要

天然产物在药物研发中发挥着重要作用,尤其是在治疗感染、癌症以及免疫抑制化合物方面。然而,天然产物的数量有限,而作为不同天然产物部分组合的数百万种杂合体却可以制备出来。这种新方法在药物和农用化学品应用的先导化合物开发中似乎非常有前景,因为几种新杂合体的生物活性超过了母体化合物。与组合化学方法相比,这一概念的优势在于杂合体具有高度多样性和内在生物活性。

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