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Preparation and pharmacological profile of 7-(α-Azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . May2003, Vol. 13 Issue 9, p1553. 3p. - Publication Year :
- 2003
-
Abstract
- Aromatase (P450 arom) is a target of pharmacological interest for the treatment of breast cancer. New series of 7-(α-azolylbenzyl)-1H-indoles and indolines were synthesized as non-steroidal inhibitors of P450 arom. Selectivity was studied towards P450 17α enzyme. The most active compound, 1-ethyl-7-[(imidazol-1-yl)(4-chlorophenyl)methyl]-1H-indole 12c exhibited promising relative potency (rp) of 336 (rp of aminoglutethimide=1) and most of the described azoles were active and selective towards P450 arom. [Copyright &y& Elsevier]
- Subjects :
- *AROMATASE
*BREAST cancer
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 13
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 9497276
- Full Text :
- https://doi.org/10.1016/S0960-894X(03)00182-3