In the study, various substituted 3-aryl-1-isoquinolinamine derivatives were shown to have excellent cytotoxicity against eight different human cancer cells (breast, prostate, colon, ovary, kidney, pancreas, glioblastoma and melanoma).

‘In this second published study, we further establish that isoquinolinamine derivatives, such as our anti-cancer compound RX-8243 – a new chemical entity – are potent anti-cancer compounds that have the potential to be developed into chemotherapeutic agents,’ said Rick Soni, President of Rexahn.

These derivatives were synthesized and evaluated through the constructed quantitative structure–activity relationship (QSAR) model and in vitro cell studies. The cytotoxic activities of new designed compounds are calculated using the constructed QSAR model and compared with actual cytotoxic data using the synthesized compounds.

Last month, Rexahn announced the publication of new preclinical data in Bioorganic & Medicinal Chemistry Letters demonstrating that RX-8243, an isoquinolinamine analogue, significantly inhibits the growth of human cancer cells, including paclitaxel (Taxol®)-resistant HCT-15 human colorectal cancer cells and the growth of tumour in an in vivo model of nude mice injected with paclitaxel-resistant HCT-15 human colorectal cancer cells.

Further reading

Yang, S.H. et al. (2010) Development of 3-aryl-1-isoquinolinamines as potent antitumor agents based on CoMFA. European Journal of Medicinal Chemistry 45, 5493–5497