Design, Synthesis and Biological Evaluation of 7-Azaindole Analogues as Novel Antiproliferative Agent and Tyrosine Protein Kinase SRC Inhibitors

Abstract

A new series of SRC inhibitors based on 7-azaindole core were designed, synthesized and evaluated for antiproliferative and antioxidant activities. All synthesized analogues of 7-azindole were characterized through ¹H and ¹³C NMR and Mass Spectrometry. Synthesized analogues were screened in vitro antiproliferative activity on the MCF-7 breast cancer cell line. Compounds 5a, 5b, 5d, 5g, and 5h showed significant results. Compound 5b was the most active in the series with a GI50 of 2.19 mM. Molecular docking studies of the most active analogues were performed to reveal the structural features responsible for their interaction with the active site of SRC. The synthesized analogues were also screened for antioxidant activity by the DPPH method. In conclusion, for the creation of novel drugs, these compounds offer promising potential.