353285-60-6Relevant academic research and scientific papers
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities
Yi, Xue-Jing,El-Idreesy, Tamer T.,Eldebss, Taha M. A.,Farag, Ahmad M.,Abdulla, Mohamed M.,Hassan, Shaimaa A.,Mabkhot, Yahia N.
, p. 832 - 843 (2016)
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.
