Synthesis, Antiproliferative, and Antioxidant Properties of Highly Functionalized Pyrazoles

Compounds 1 showed promising antioxidant activity by inhibiting ROS formation in platelet. The substitution of the catechol moiety modulates the ability of the compounds to block ROS formation. To further extend the structure-activity relationships (SARs) and evaluate the insertion of an additional substituent on the pyrazole ring, derivatives 2 and 3 were designed, synthesized and characterized. The adopted synthetic strategy involved a divergent approach starting from the common intermediates A. The synthesis of pyrazoles A was carried out by a sequential, one-pot procedure which represents a cheaper alternative either in terms of time or cost. The derivatization of either the ester or the amino functionalities led to the formation of derivatives 2 and 3, respectively.