Literature

Abstract

This study is concerned with the implementation of structure-based techniques for the design of new heterocyclic compounds based on pseudosaccharine scaffold with protein kinase inhibition activity. This nucleus was exploited based on the well-known quinazoline core and its interactions with several protein kinases. Two series of compounds employing this new scaffold were synthesized and evaluated at enzymatic and cellular levels. Compound 9b displayed broad spectrum antiproliferative activity on NCI 60-cell lines panel with mean GI50 of 5.4 μM. Investigation of the molecular mechanism showed probable inhibitory activity against Src kinase.

DOI： 10.1016/j.ejmech.2012.09.039

Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors

European Journal of Medicinal Chemistry 2013.0

Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors

Bioorganic & Medicinal Chemistry 2016.0

The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton

Bioorganic & Medicinal Chemistry 2019.0

Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors

Bioorganic & Medicinal Chemistry Letters 2012.0

Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening

Bioorganic & Medicinal Chemistry Letters 2016.0

Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors