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 IC value of 0.0023 ± 0.0002 μm compared to letrozole with IC of 0.0028 ± 0.0006 μm. In addition, compounds 26 and 36 exhibit good inhibition activities close to letrozole with IC 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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