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

Dawei Ma, Tao Zhang, Guoqiang Wang, Alan P. Kozikowski, Nancy E. Lewin, Peter M. Blumberg

Research output: Contribution to journalArticlepeer-review

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 PKCα, δ, and ε, respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.

Original languageEnglish (US)
Pages (from-to)99-101
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number2
DOIs
StatePublished - Jan 22 2001

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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