Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety

Autor:	Maxwell Pan, Maryanne Covington, Peggy Scherle, Eric Shi, Wenqing Yao, Yun-Long Li, Yanlong Li, David M. Burns, Steve Friedman, Brian Metcalf
Rok vydání:	2009
Předmět:	Receptor ErbB-2 medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Humans Moiety Structure–activity relationship Collagenases Protein Kinase Inhibitors Molecular Biology chemistry.chemical_classification Hydroxamic acid Organic Chemistry Sheddase Enzyme chemistry Microsomes Liver Molecular Medicine Carbamates Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:5037-5042
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2009.07.052
Popis:	A novel series of carbamates was discovered as potent and selective HER-2 sheddase inhibitors. Significant enhancement in potency and selectivity was achieved through attenuating the P1 moiety, which was conventionally believed to be exposed to solvent.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64c3af5b5030ff053a046c46c77f1051 https://doi.org/10.1016/j.bmcl.2009.07.052 Zobrazit plný text záznamu Full Text from ScienceDirect