Structure-based hybridization of the bioactive natural products rhizonin A and ternatin leading to a selective fat-accumulation inhibitor against 3T3-L1 adipocytes.

Structure-based hybridization of the bioactive natural products rhizonin A and ternatin leading to a selective fat-accumulation inhibitor against 3T3-L1 adipocytes.
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DOI:
10.1016/j.bmcl.2008.11.109
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发表时间:
2009-02
影响因子:
2.7
通讯作者:
K. Shimokawa;Kaoru Yamada;D. Uemura
K. Shimokawa;Kaoru Yamada;D. Uemura
中科院分区:
医学4区
文献类型:
--
作者:
K. Shimokawa;Kaoru Yamada;D. Uemura

文献摘要

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基于天然存在的环状七肽rhizonin A和ternatin之间的结构相似性,设计了两个新的类似物。评估了合成类似物对3 T3-L1脂肪细胞的脂肪蓄积抑制作用,与母体化合物根茎皂苷A相比,这导致发现了有效的选择性脂肪蓄积抑制剂。
Based on the structural similarity between the naturally occurring cyclic heptapeptides rhizonin A and ternatin, two novel analogues were designed. The synthetic analogues were assessed with regard to their fat-accumulation inhibitory effect against 3T3-L1 adipocytes, and this led to the discovery of a potent and selective fat-accumulation inhibitor compared to the parent compound rhizonin A.