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二酰基甘油的构象受限类似物。19. 带有N-羟基酰胺侧链的二酰基甘油内酯的合成及蛋白激酶C结合亲和力

Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.

作者信息

Choi Yongseok, Kang Ji-Hye, Lewin Nancy E, Blumberg Peter M, Lee Jeewoo, Marquez Victor E

机构信息

Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute at Frederick, National Institutes of Health, Frederick, Maryland 21702, USA.

出版信息

J Med Chem. 2003 Jun 19;46(13):2790-3. doi: 10.1021/jm030082c.

DOI:10.1021/jm030082c
PMID:12801241
Abstract

The structures of N-hydroxylamides 1a and 1b, previously reported by Lee et al. in J. Med. Chem. 2001, 44, 4309-4312 as strong protein kinase C (PK-C) ligands, were incorrect and correspond instead to esters 2a and 2b, respectively. Here, we report the synthesis and complete characterization of 1a and 1b together with the associated biological activity in terms of PK-C binding affinity.

摘要

李等人于2001年发表在《药物化学杂志》第44卷第4309 - 4312页上的文章中，曾将N - 羟基酰胺1a和1b作为强效蛋白激酶C（PK - C）配体报道，但它们的结构是错误的，实际上分别对应酯类2a和2b。在此，我们报道了1a和1b的合成、完整表征以及它们在PK - C结合亲和力方面的相关生物活性。

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