Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.

Autor: Tian Y; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address: yuan.tian2@merck.com., Ma Y; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA., Gibeau CR; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA., Lahue BR; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA., Shipps GW Jr; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA., Strickland C; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA., Bogen SL; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Jun 01; Vol. 26 (11), pp. 2735-8. Date of Electronic Publication: 2016 Mar 23.
DOI: 10.1016/j.bmcl.2016.03.078
Abstrakt: Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53-hDM2 inhibitors was conducted. A structure-activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.
(Copyright © 2016 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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