Synthesis of some novel androstanes as potential aromatase inhibitors
Autor: | Mange Ram Yadav, Rolf W. Hartmann, Rajani Giridhar, Jörg Haupenthal, Prafulla M. Sabale, Christina Zimmer |
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Rok vydání: | 2011 |
Předmět: |
Nitrile
Stereochemistry medicine.drug_class Clinical Biochemistry Pyrazole Biochemistry Structure-Activity Relationship chemistry.chemical_compound Endocrinology medicine Humans Structure–activity relationship Hydrazine (antidepressant) Isoxazole Aromatase Molecular Biology Pharmacology Aromatase inhibitor biology Aromatase Inhibitors Organic Chemistry Isoxazoles Kinetics Fadrozole chemistry biology.protein Pyrazoles Androstanes Protein Binding medicine.drug |
Zdroj: | Steroids. 76:464-470 |
ISSN: | 0039-128X |
Popis: | Novel pyrazole and isoxazole derivatives (6-9) were synthesized as a aromatase inhibitors. Pyrazole was synthesized from hydrazine hydrate and isoxazoles from hydroxylamine hydrochloride under different conditions. Molecular docking studies were carried out for the synthesized compounds. The best score was obtained for the compound (9) followed by compound (6) while compound (8) afforded poorest of the score. Aromatase inhibitory activity for compound (6) having pyrazole ring at 2,3 position showed highest activity followed by nitrile derivative (9). Isomeric forms of isoxazole (7 and 8) showed very poor activity compared to fadrozole and aminoglutethimide. Preliminary kinetic studies have shown that both of the active compounds (6 and 9) are reversible inhibitors of the enzyme. |
Databáze: | OpenAIRE |
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