title: Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
abstract: 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.
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors.forename: Yao
authors.initials: Y
authors.lastname: Ma
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors.forename: Brian R
authors.initials: BR
authors.lastname: Lahue
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors.forename: Craig R
authors.initials: CR
authors.lastname: Gibeau
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors.forename: Gerald W
authors.initials: GW
authors.lastname: Shipps
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
authors.forename: Stéphane L
authors.initials: SL
authors.lastname: Bogen
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
authors.forename: Yaolin
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
authors.forename: Zhuyan
authors.initials: Z
authors.lastname: Guo
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Guzi
keywords: HDM2; MDM2; p53; protein−protein interaction; small molecule inhibitor; substituted piperidine