title: Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
abstract: A series of C-H functionalisation plate-based chemical screens and other C-H activation protocols were developed for the chemical diversification of drug molecules. In this Letter, metalloporphyrin and other catalytic oxidation systems are described in addition to chlorination. Mifepristone and antalarmin are used as substrates. The products obtained and the biological data demonstrate the potential utility of this approach.
authors: Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. mabidmasood@gmail.com
authors: M
authors: M
authors: Abid Masood
authors: Elizabeth
authors: E
authors: Farrant
authors: Inaki
authors: I
authors: Morao
authors: Marc
authors: M
authors: Bazin
authors: Manuel
authors: M
authors: Perez
authors: Mark E
authors: ME
authors: Bunnage
authors: Sally-Ann
authors: SA
authors: Fancy
authors: Torren
authors: T
authors: Peakman
mesh_terms: D032701:Biomimetics; D002244:Carbon / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002713:Chlorine / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D006859:Hydrogen / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008665:Metalloporphyrins / Q000737:chemistry; D008670:Metals / Q000737:chemistry; D008862:Microsomes, Liver / Q000187:drug effects; D015735:Mifepristone / Q000494:pharmacology*; D008956:Models, Chemical; D010100:Oxygen / Q000737:chemistry; D011743:Pyrimidines / Q000494:pharmacology*; D011758:Pyrroles / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D008665:Metalloporphyrins; D008670:Metals; D011743:Pyrimidines; D011758:Pyrroles; C103016:antalarmin; D015735:Mifepristone; D002713:Chlorine; D002244:Carbon; D006859:Hydrogen; D010100:Oxygen