Lead Diversification 2: application to P38, gMTP and lead compounds

M Abid Masood; Marc Bazin; Mark E Bunnage; Andrew Calabrese; Mark Cox; Sally-Ann Fancy; Elizabeth Farrant; David W Pearce; Manuel Perez; Laure Hitzel; Torren Peakman

doi:10.1016/j.bmcl.2011.11.033

Lead Diversification 2: application to P38, gMTP and lead compounds

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1255-62. doi: 10.1016/j.bmcl.2011.11.033. Epub 2011 Nov 17.

Authors

M Abid Masood¹, Marc Bazin, Mark E Bunnage, Andrew Calabrese, Mark Cox, Sally-Ann Fancy, Elizabeth Farrant, David W Pearce, Manuel Perez, Laure Hitzel, Torren Peakman

Affiliation

¹ Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. [email protected]; [email protected]

PMID: 22172703
DOI: 10.1016/j.bmcl.2011.11.033

Abstract

Lead Diversification is a new technology platform developed at Pfizer for the functionalization of drug molecules using C-H activation. We describe its application to some drug programs such as P38 and gMTP and the development of some new plate based screens including a fluorination screen.

MeSH terms

Acetylmuramyl-Alanyl-Isoglutamine / analogs & derivatives
Acetylmuramyl-Alanyl-Isoglutamine / chemistry
Acetylmuramyl-Alanyl-Isoglutamine / pharmacology*
Humans
Molecular Structure
Organometallic Compounds / chemical synthesis
Organometallic Compounds / chemistry
Organometallic Compounds / pharmacology*
Palladium / chemistry*
Protein Kinase Inhibitors / chemical synthesis
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology*
Structure-Activity Relationship
p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
p38 Mitogen-Activated Protein Kinases / metabolism

Substances

Organometallic Compounds
Protein Kinase Inhibitors
Acetylmuramyl-Alanyl-Isoglutamine
Palladium
p38 Mitogen-Activated Protein Kinases