Medicinal Chemistry

Synthesis of 3-Arylidene and 3-Arylimine Oxindole Derivatives and Evaluation of Their Src Kinase Inhibitory and Antiproliferative Activities

Abstract

Shaya Mokhtari, Amir Nasrolahi Shirazi, Rakesh Kumar Tiwari, Keykavous Parang and Farzad Kobarfard

A number of novel 3-arylilidene and 3-arylimine-2-oxindole derivatives were synthesized, and their Src kinase inhibitory activities and antiproliferative activities were evaluated. Several compounds exhibited Src kinase inhibitory activitywith IC50 values in the range of 5.3 to 211.8 μM. Compound b11 in 3-arylimine-2-oxindoles showed IC50 values of 5.3 μM against Src kinase. Compounds a8, a20, a38, and b15 showed consistently>50% proliferation inhibition against all three cancer celllines at a concentration of 50 μM.