Synthesis and evaluation of C3 substituted chalcone‐based derivatives of 7‐azaindole as protein kinase inhibitors

Abstract

Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty-three 7-azaindole-chalcone hybrids (5a-w) were synthesized and evaluated as potential protein kinase inhibitors. Analyses of structure-activity relationships revealed that some of these compounds exhibit significant activity against Haspin kinase, with compounds 5f and 5q exhibiting IC 50 values of 0.47 and 0.41 µM, respectively. Furthermore, 5f also inhibits cyclin-dependent kinase 9 (CDK9/CyclinT) in a micromolar potency (IC 50 = 2.26 µM). This novel dual-target inhibitor is a promising lead for the development of chemopreventive/chemotherapeutic agents.

Laser spectroscopic characterization of supersonic jet cooled 2,7-diazaindole

“…[23][24][25] Its synthetically designed derivatives have been employed as potential protein kinase inhibitors which are important drug targets in various oncology studies. [26][27][28][29][30] The molecules have also been utilized in the design of antitumor, anti-inflammatory, antibacterial, antimalarial, antimicrobial, antifungal, antituberculosis, and anticancer agents. [31][32][33][34][35][36] Recent studies have shown that Janus Kinase (JAK) inhibitors, such as Peficitinib, containing an azaindole moiety, have shown promising results in COVID-19 treatment.…”

Laser Spectroscopic Characterization of Supersonic Jet Cooled 2,7-Diazaindole (27DAI)

“…[23][24][25] Its synthetically designed derivatives have been employed as potential protein kinase inhibitors which are important drug targets in various oncology studies. [26][27][28] They work as an excellent coronary vasodilator and hypotensive agents. 29,30 They are also utilized in the designing of antitumor, antiinflammatory, antibacterial, antimalarial, antimicrobial, antifungal, antituberculosis, and anticancer properties.…”