A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
| Autor: | Zhihua Sui, George F. Allan, Do Won Hahn, Amy Musto, James J. Fiordeliso, James C. Lanter |
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| Rok vydání: | 2006 |
| Předmět: |
Indoles
Bicalutamide Imidazolidinone Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science urologic and male genital diseases Antiandrogen Ligands Biochemistry Androgen receptor binding chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Moiety Animals Molecular Biology Indole test Chemistry Methanol Organic Chemistry Rats Androgen receptor Receptors Androgen Molecular Medicine Bioisostere medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 16(21) |
| ISSN: | 0960-894X |
| Popis: | Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiety in the parent compound. Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain. |
| Databáze: | OpenAIRE |
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