Literature DB >> 11206480

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

D Ma1, T Zhang, G Wang, A P Kozikowski, N E Lewin, P M Blumberg.   

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.

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Year:  2001        PMID: 11206480     DOI: 10.1016/s0960-894x(00)00609-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Identification of a small molecule activator of novel PKCs for promoting glucose-dependent insulin secretion.

Authors:  Shuai Han; Heling Pan; Jianhua Zhang; Li Tan; Dawei Ma; Junying Yuan; Jia-Rui Wu
Journal:  Cell Res       Date:  2010-09-28       Impact factor: 25.617

2.  Solventless lactam synthesis by intramolecular cyclizations of alpha-iminoester derivatives under microwave irradiation.

Authors:  Fatima-Zohra Zradni; Jack Hamelin; Aicha Derdour
Journal:  Molecules       Date:  2007-03-12       Impact factor: 4.411

Review 3.  PKC in Regenerative Therapy: New Insights for Old Targets.

Authors:  Marta Rui; Rita Nasti; Emanuele Bignardi; Serena Della Volpe; Giacomo Rossino; Daniela Rossi; Simona Collina
Journal:  Pharmaceuticals (Basel)       Date:  2017-05-18
  3 in total

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