Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy.

Autor: Chekler EL; Department of Chemistry., Kiselyov AS; Department of Chemistry., Ouyang X; Department of Chemistry., Chen X; Department of Chemistry., Pattaropong V; Department of Chemistry., Wang Y; Department of Cell Biology., Tuma MC; Department of Cell Biology., Doody JF; Department of Cell Biology.
Jazyk: angličtina
Zdroj: ACS medicinal chemistry letters [ACS Med Chem Lett] 2010 Aug 20; Vol. 1 (9), pp. 488-92. Date of Electronic Publication: 2010 Aug 20 (Print Publication: 2010).
DOI: 10.1021/ml1001568
Abstrakt: In an effort to develop potent, orally bioavailable compounds for the treatment of neoplastic diseases, we developed a class of dual VEGFR-2 kinase and tubulin inhibitors. Targeting the VEGFR receptor kinase and tubulin structure allows for inhibition of both tumor cells and tumor vasculature. Previously, a combination of two compounds, a VEGF receptor tyrosine kinase inhibitor and tubulin agent, was demonstrated to produce an enhanced antitumor response in animal studies. We have reaffirmed their results, with the added benefit that both activities are found in one compound.
Databáze: MEDLINE