A natural love of natural products.

A natural love of natural products.
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DOI:
10.1021/jo800239a
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发表时间:
2008-06-06
期刊:
The Journal of organic chemistry
影响因子:
--
通讯作者:
Kingston DG
Kingston DG
中科院分区:
其他
文献类型:
--
作者:
Kingston DG

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回顾了作者小组最近关于天然产物化学的研究,这些研究导致获得了 ACS Ernest Guenther 天然产物化学奖。 REDOR NMR和合成研究将T-紫杉醇构象确定为具有生物活性的微管蛋白结合构象,并且这些结果通过化合物的合成得到证实,这些化合物的活性或缺乏活性显然取决于它们是否可以采用T-紫杉醇构象。对埃博霉素的类似研究表明,当前的微管蛋白结合模型需要修改。还介绍了苏里南和马达加斯加的天然产物发现和生物多样性保护的例子,得出的结论是天然产物化学将继续为药物发现做出重大贡献。
Recent research on the chemistry of natural products from the author’s group that led to the receipt of the ACS Ernest Guenther Award in the Chemistry of Natural Products is reviewed. REDOR NMR and synthetic studies established the T-taxol conformation as the bioactive tubulin-binding conformation, and these results were confirmed by the synthesis of compounds which clearly owed their activity or lack of activity to whether or not they could adopt the T-taxol conformation. Similar studies with the epothilones suggest that the current tubulin-binding model needs to be modified. Examples of natural products discovery and biodiversity conservation in Suriname and Madagascar are also presented, and it is concluded that natural products chemistry will continue to make significant contributions to drug discovery.
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