Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.
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Wang R, Shi HF, Zhao JF, He YP, Zhang HB, Liu JP
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.
Bioorg Med Chem Lett. 2013 Mar 15;23(6):1760-2. doi: 10.1016/j.bmcl.2013.01.045. Epub 2013 Jan 26.
- PubMed ID
- 23403081 [ View in PubMed]
- Abstract
A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Letrozole Cytochrome P450 19A1 IC 50 (nM) 17 N/A N/A Details