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 journalArticle

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
Externally publishedYes

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Alkylation
Protein Kinase C
Isoenzymes
Carrier Proteins

ASJC Scopus subject areas

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

Cite this

Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C. / Ma, Dawei; Zhang, Tao; Wang, Guoqiang; Kozikowski, Alan P.; Lewin, Nancy E.; Blumberg, Peter M.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 2, 22.01.2001, p. 99-101.

Research output: Contribution to journalArticle

Ma, Dawei ; Zhang, Tao ; Wang, Guoqiang ; Kozikowski, Alan P. ; Lewin, Nancy E. ; Blumberg, Peter M. / Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 2. pp. 99-101.
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