Abstract
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.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.