Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
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Abid Masood M, Farrant E, Morao I, Bazin M, Perez M, Bunnage ME, Fancy SA, Peakman T
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
Bioorg Med Chem Lett. 2012 Jan 1;22(1):723-8. doi: 10.1016/j.bmcl.2011.10.066. Epub 2011 Oct 25.
- PubMed ID
- 22104142 [ View in PubMed]
- 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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Progesterone receptor IC 50 (nM) 10 N/A N/A Details