179246-81-2Relevant academic research and scientific papers
Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines
Asquith, Christopher R.M.,Fleck, Neil,Torrice, Chad D.,Crona, Daniel J.,Grundner, Christoph,Zuercher, William J.
, p. 2695 - 2699 (2019/08/07)
We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline scaffold arrays yielded compounds with high potency and the identification of 6,7-dimethoxy-N-(4-((4-methylbenzyl)oxy)phenyl)quinolin-4-amine (34) with an MIC90 value of 0.63–1.25 μM. We also defined a series of key structural features, including the benzyloxy aniline and the 6,7-dimethoxy quinoline ring, that are important for Mtb inhibition. Importantly the compounds showed very limited toxicity and scope for further improvement by iterative medicinal chemistry.
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors
Zhang, Yue-Mei,Cockerill, Stuart,Guntrip, Stephen B.,Rusnak, David,Smith, Kathryn,Vanderwall, Dana,Wood, Edgar,Lackey, Karen
, p. 111 - 114 (2007/10/03)
A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC50 values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.
