Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs
US7595326B2 · kind B2 · utility
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Key dates
| Filing date | Feb 9, 2007 |
| Grant date | Sep 29, 2009 |
| Priority date | — |
| Expiry date | Feb 9, 2027 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D239/38
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.
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