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1.
Bioorg Med Chem Lett ; 20(22): 6394-9, 2010 Nov 15.
Article in English | MEDLINE | ID: mdl-20932747

ABSTRACT

We have designed and synthesized analogues of compound C, a non-specific inhibitor of 5'-AMP-activated protein kinase (AMPK), using a computational fragment-based drug design (FBDD) approach. Synthesizing only twenty-seven analogues yielded a compound that was equipotent to compound C in the inhibition of the human AMPK (hAMPK) α2 subunit in the heterotrimeric complex in vitro, exhibited significantly improved selectivity against a subset of relevant kinases, and demonstrated enhanced cellular inhibition of AMPK.


Subject(s)
AMP-Activated Protein Kinases/antagonists & inhibitors , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/pharmacology , Drug Design , Humans , Models, Molecular , Phosphorylation , Structure-Activity Relationship
2.
Org Biomol Chem ; 1(17): 3007-9, 2003 Sep 07.
Article in English | MEDLINE | ID: mdl-14518121

ABSTRACT

1,2-Disubstituted olefins bearing an acetamide group were found to undergo intramolecular Kulinkovich-de Meijere cyclopropanation in moderate yield but almost complete diastereoselectivity.

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