Bryostatins are a class of macrocyclic lactones with a unique polyacetate backbone. Currently, there are 20 known exceptionally potent anti-neoplastic natural compounds belonging to the Bryostatin family. Bryostatin 1 has undergone Phase II clinical trials for treatment of cancer, and is now in combination therapy trials.

Bryostatins modified at the C-26 position show a significantly increased therapeutic window versus unmodified Bryostatin 1.

Potential Applications

This new development has applications in:

• Anti-cancer agents with enhanced therapeutic windows.

Benefits and Advantages

• Diversity – Numerous modifications are proposed.
• Efficacy – Testing results demonstrate diminished toxicity for modified Bryostatins, with equivalent antineoplastic activity.
• Synthesis – Bryostatins are both available from total synthesis and from extraction from biological material.