期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 9, 页码 488-492出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml1001568
关键词
Tubulin; angiogenesis; VEGFR; tumor vasculature; antimitotic; vascular disrupting agent
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.
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