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

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mifepristone	Progesterone receptor	IC 50 (nM)	10	N/A	N/A	Details