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Updated: Mar 15, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase
Xue-Jing Yi1, Tamer T El-Idreesy2,3, Taha M A Eldebss4
1Yueyang Vocational Technical College, Yueyang, China.
Abstract:
A new series derived from 4-(2-chloroacetyl)-1,2-dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one was synthesized, characterized and its pharmacological activity toward aromatase enzyme inhibition was screened and compared to the reference native ligand letrozole. The most active compound of the series was 16, showing IC50 value of 0.0023 ± 0.0002 μm compared to letrozole with IC50 of 0.0028 ± 0.0006 μm. In addition, compounds 26 and 36 exhibit good inhibition activities close to letrozole with IC50 values 0.0033 ± 0.0001 and 0.0032 ± 0.0003 μm, respectively. Moreover, molecular docking studies were conducted to support the findings.
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