Antifolate agents: a patent review (2010 - 2013).

Area of Science:

• Biochemistry
• Medicinal Chemistry
• Drug Discovery

Background:

• The folate biosynthetic pathway is vital for synthesizing essential cellular components, particularly in rapidly dividing cells.
• This pathway presents druggable targets for treating cancer, infectious diseases, and autoimmune disorders.
• Antifolate compounds are critical for impacting these disease states.

Purpose of the Study:

• To review recent advancements in antifolate compound development.
• To evaluate patent literature from 2010-2013 concerning inhibitors of the folate biosynthetic pathway.
• To identify promising drug targets within the folate pathway for therapeutic intervention.

Main Methods:

• Focused evaluation of patent literature from 2010 to 2013.
• Identification of compounds inhibiting known targets in the folate biosynthetic pathway.
• Analysis of structure-based drug design approaches.

Main Results:

• The folate pathway remains a well-validated target for drug discovery.
• Dihydrofolate reductase and thymidylate synthase are key targets for cancer and infectious disease therapies.
• New targets within the purine biosynthetic pathway are being explored.

Conclusions:

• The folate pathway continues to generate significant interest for new drug discovery.
• Structure-based drug design is central to modern antifolate drug development.
• Enzymes like dihydrofolate reductase and thymidylate synthase remain highly attractive targets.