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Antifolate agents: a patent review (2006 - 2010).
Dennis L Wright1, Amy C Anderson
1University of Connecticut, Department of Pharmaceutical Sciences , 69 N. Eagleville Rd. Storrs, CT, USA.
Expert Opinion on Therapeutic Patents
|May 31, 2011
Summary
Researchers are developing new antifolate drugs targeting the folate pathway for cancer and infections. Recent patents show novel compounds and improved drug properties, with X-ray crystallography guiding discovery.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Biochemistry
Background:
- Drugs targeting the folate pathway have been used for over 50 years.
- Anticancer, antimicrobial, and immunomodulatory agents are key applications.
- Novel antifolate discovery is a strategic focus in research and industry.
Purpose of the Study:
- To review patent literature on small molecule inhibitors of folate biosynthesis.
- Focus on patents published between 2006 and 2010.
- Identify novel antifolate scaffolds and design strategies.
Main Methods:
- Literature review of patent filings.
- Analysis of small molecule inhibitors.
- Focus on enzymatic targets within the folate biosynthetic pathway.
Main Results:
- Identification of novel antifolate scaffolds.
- Discovery of antifolates with enhanced drug-like properties.
- Emergence of new strategies for targeting cancer cells.
Conclusions:
- Antifolates remain a critical area for anticancer and antimicrobial drug development.
- High-resolution structural information, particularly X-ray crystallography, is vital for designing potent and selective compounds.
- New antifolate structures reported in patents hold promise for future therapeutics.
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