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Bioorg Med Chem Lett. 2000 Sep 18;10(18):2087-90.

Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.

Author information

1
Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University, Japan.

Abstract

To investigate the role of the amide group of (-)-indolactam-V (1) on PKC binding, we synthesized (-)-indothiolactam-V (2), a new thioamide analogue of 1, by microbial conversion using Streptomyces blastmyceticum. Compounds 2 and 1 showed similar binding affinities to conventional PKCs but 2 had lower affinities to novel PKCs, suggesting that novel PKCs recognize amide modifications more effectively than conventional PKCs.

PMID:
10999477
DOI:
10.1016/s0960-894x(00)00411-x
[Indexed for MEDLINE]

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