Synthesis and biological evaluation of novel isothiazoloquinoline quinone analogues.

ID: ALA4622930

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of novel isothiazoloquinoline quinone analogues.

Authors: Chen L, Xie YZ, Luo ZY, Liu LJ, Zou ZZ, Liu HD, Kong FR, Hao Y, Gao JL, Wang LL, Ma DY, Liu SY.

Abstract: Natural quinones and their analogues have attracted growing attention because of their novel anticancer activities. A series of novel isothiazoloquinoline quinone analogues were synthesized and evaluated for antitumor activities against four different kind of cancer cells. Among them, isothiazoloquinolinoquinones inhibited cancer cells proliferation effectively with IC₅₀ values in the nanomolar range, and isothiazoloquinolinoquinone 13a induced the cell apoptosis. Further exploration of possible mechanism of action indicates that 13a not only activates ROS production through NQO1-directed redox cycling but also inhibits the phosphorylation of STAT3. These findings indicate that 13a has potential use for the development of new skeleton drug candidate as an efficient substrate of NQO1 and STAT3 inhibitor.

CiteXplore: 32631508

DOI: 10.1016/j.bmcl.2020.127286

Patent ID: ┄