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Published on: August 1, 2019
Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy
Eugene L Piatnitski Chekler1, Alexander S Kiselyov1, Xiaohu Ouyang1
1Department of Chemistry.
Abstract:
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.
Insights
Researchers developed a novel compound that inhibits both vascular endothelial growth factor receptor 2 (VEGFR-2) kinase and tubulin. This dual-action drug targets tumor cells and vasculature, offering a new strategy for cancer treatment.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Neoplastic diseases require novel therapeutic strategies.
- Targeting both tumor cells and vasculature is a promising approach.
- Previous studies showed combined VEGFR inhibitor and tubulin agent efficacy.
Purpose of the Study:
- To develop potent, orally bioavailable compounds for cancer treatment.
- To create a single compound with dual VEGFR-2 kinase and tubulin inhibitory activity.
- To inhibit both tumor cell proliferation and tumor vasculature formation.
Main Methods:
- Development of a novel class of dual inhibitors.
- In vitro and in vivo testing of compound efficacy.
- Pharmacokinetic and pharmacodynamic studies for oral bioavailability.
Main Results:
- Successful development of dual VEGFR-2 kinase and tubulin inhibitors.
- Demonstration of potent antitumor activity in preclinical models.
- Confirmation that a single compound can possess both inhibitory activities.
Conclusions:
- Dual inhibition of VEGFR-2 kinase and tubulin is a viable strategy for cancer therapy.
- The developed compounds show potential as orally bioavailable anticancer drugs.
- This approach offers a simplified and potentially more effective treatment option.
