Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.

Autor: Ma Y; Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Lahue BR; Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Gibeau CR; Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Shipps GW Jr; Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Bogen SL; Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Wang Y; Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Guo Z; Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States., Guzi TJ; Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Jazyk: angličtina
Zdroj: ACS medicinal chemistry letters [ACS Med Chem Lett] 2014 Feb 24; Vol. 5 (5), pp. 572-5. Date of Electronic Publication: 2014 Feb 24 (Print Publication: 2014).
DOI: 10.1021/ml500019s
Abstrakt: Introduction of an aliphatic side chain to a key position of a novel piperidine-based HDM2 inhibitor scaffold resulted in significant potency gains, enabling further series progression.
Databáze: MEDLINE