e-7010 and verubulin
e-7010 has been researched along with verubulin* in 1 studies
Other Studies
1 other study(ies) available for e-7010 and verubulin
| Article | Year |
|---|---|
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
As a continuation of our structure-activity relationship (SAR) studies on 4-anilinoquinazolines as potent apoptosis inducers and to identify anticancer development candidates, we explored the replacement of the 2-Cl group in our lead compound 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (6b, EP128265, MPI-0441138) by other functional groups. This SAR study and lead optimization resulted in the identification of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine (6h, EP128495, MPC-6827) as an anticancer clinical candidate. Compound 6h was found to be a potent apoptosis inducer with EC(50) of 2 nM in our cell-based apoptosis induction assay. It also has excellent blood brain barrier penetration, and is highly efficacious in human MX-1 breast and other mouse xenograft cancer models. Topics: Animals; Antineoplastic Agents; Apoptosis; Blood-Brain Barrier; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Mice; Neoplasm Transplantation; Quinazolines; Structure-Activity Relationship; Transplantation, Heterologous | 2009 |