Biologically active triterpenoid derivatives III

Introduction: 
Triterpenoids are naturally occurring substances showing a large range of biological activities, including strong cytotoxic activity. This would make them suitable for use as pharmaceuticals.
Technology description: 
The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in therapy. Preferably, the compound may be used for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation and acetylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia).
Development status: 
Laboratory scale, data on cell lines, limited ADME/Tox data, in vivo pharmacology and pharmacodynamics.
Advantages: 
The invention provides a novel class of compounds possessing a cytotoxic activity to a wide range of tumor cell lines. Our recent data demonstrate that selected compounds covered by these patents are hedge-hog inhibitors, pro-apoptotic compounds inducing selective release of cytochrome c from tumor cells, tubulin polymerization inhibitors, hemoxygenase I inducers, HIV maturation inhibitors, etc. These compounds will be useful as medicaments for the treatment of cancer and other diseases connected with abnormal proliferation and/or HIV infection.
Commercial offer: 
Exclusive/non-exclusive licence to the patents, related know-how and data
Papers: 
Kvasnica, M., Urban, M., Dickinson, N. J., Sarek, J. Pentacyclic triterpenoids with nitrogen- and sulfur-containing heterocycles: synthesis and medicinal significance. Nat Prod Rep. 2015 Jun 1. PubMed PMID: 26030604 Borkova, L., Jasikova, L., Rehulka, J., Frisonsova, K., Urban, M., Frydrych, I., Popa, I.,Hajduch, M., Dickinson, N. J., Vlk, M., Dzubak, P., Sarek, J. Synthesis of cytotoxic 2,2-difluoroderivatives of dihydrobetulinic acid and allobetulin and study of their impact on cancer cells. Eur J Med Chem. 2015 May 26, doi: 10.1016/j.ejmech.2015.03.068. Epub 2015 Apr 1. PubMed PMID: 25942059. Sarek, J., Klinot, J., Dzubak, P., Klinotova, E., Noskova, V., Krecek, V., Korinkova, G., Thomson, J. P., Janostakova, A., Wang, S. D., Parsons, S., Fischer, P. M., Zhelev, N. Z., Hajduch, M. New lupane derived compounds with pro-apoptotic activity in cancer cells: Synthesis and structure - Activity relationships. J. Med. Chem. 2003, 46, 5402.
IP protection: 
US 7,041,701 US 7,749,988
Technology/IP owners: 
Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University, Olomouc Charles University Prague Cyclacel Ltd.
Contact: 
More information is available upon signing a CDA/NDA. Please contact IMTM´s director (director@imtm.upol.cz) or the technology transfer office (tto@imtm.upol.cz).