Anti-tumor triterpenoids substituted with nitrogen substituents

Triterpenoids are natural compounds with a number of biological activities including anticancer. Most of the triterpenoids are not sufficiently water soluble, which makes the biological tests difficult and also is a reason for low bioavailability. Therefore, it is important to improve the solubility by modifying the compounds with polar functional groups such as quaternary ammonium salts.

The invention is based on the introduction of quaternary ammonium salts into the triterpenic structure of active compounds. Those ammonium salts are connected to the 18-carboxylic acid via alkyl-ester linker. Compounds containing both aliphatic and aromatic quaternary ammonium salts were studied and patented and they showed high in vitro cytotoxic activities.

The invention provides a large group of novel compounds active on broad spectrum of cancer cell lines. New anti-cancer pharmaceu¬ticals can be based on the invention as well as abnormal proliferation therapeutics.

CZ 301158

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