Literature

Abstract

Because both c-Src and iNOS are key regulatory enzymes in tumorigenesis, a new series of 4-heterocycle amine-3-quinolinecarbonitriles as potent dual inhibitors of both enzymes were designed, synthesized and evaluated as multiple targets agents in cancer therapy. All compounds were evaluated by two related enzyme inhibition assays and an anti-proliferation assay in vitro. The results showed that most compounds inhibited c-Src and iNOS well. The best compound 8 inhibited both enzymes with the IC(50) values of 34.8 nM and 26.7 microM. Several compounds also showed moderate anti-proliferation at 10 microM against colon and liver cancer cell lines.

DOI： 10.1016/j.bmcl.2008.10.006

The design, synthesis and biological evaluation of 7-alkoxy-4-heteroarylamino-3-cyanoquinolines as dual inhibitors of c-Src and iNOS

Bioorganic & Medicinal Chemistry Letters 2008.0

Design and synthesis of 7-alkoxy-4-heteroarylamino-3-quinolinecarbonitriles as dual inhibitors of c-Src kinase and nitric oxide synthase

Bioorganic & Medicinal Chemistry 2008.0

Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: Dual inhibitors of EGFR and Src protein tyrosine kinases

European Journal of Medicinal Chemistry 2012.0

Pyrroloquinolinone-based dual topoisomerase I/II inhibitor

European Journal of Medicinal Chemistry 2014.0

Synthesis and antitumor activities of certain novel 2-amino-9-(4-halostyryl)-4H-pyrano[3,2-h]quinoline derivatives

Medicinal Chemistry Research 2012.0

Design, Synthesis, and Structure–Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer