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Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.

Abstract：

:7-Methoxy-8-decynyl-benzolactam-V8 4 is synthesized using a catalytic asymmetric alkylation reaction as a key step. This compound shows potent activity to three PKC isozymes tested (Ki =45.6, 91.1, and 121.3 nM to PKCalpha, delta, and epsilon, respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ma D,Zhang T,Wang G,Kozikowski AP,Lewin NE,Blumberg PM

doi

10.1016/s0960-894x(00)00609-0

subject

Has Abstract

pub_date

2001-01-22 00:00:00

pages

99-101

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960894X00006090

journal_volume

11

pub_type

杂志文章

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