Rexahn announces publication of 3-aryl-1-isoquinolinamines preclinical data

Oct 19 2010

Rexahn Pharmaceuticals, Inc. (NYSE Amex: RNN), a clinical stage pharmaceutical company developing and commercializing potential best in class oncology and CNS therapeutics, today announced the publication of new preclinical data on the development of 3-aryl-1-isoquinolinamines in the European Journal & Medicinal Chemistry [45:5493-5497, 2010].

“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”

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, melanoma). These derivatives were synthesized and evaluated through the constructed QSAR (quantitative structure-activity relationship) model and in vitro cell studies. QSAR technique is used in drug design and virtual screening to find lead compounds. The cytotoxic activities of new designed compounds are calculated using the constructed QSAR model and compared with actual cytotoxic data using the synthesized compounds.

"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.

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 tumor in in vivo model of nude mice injected with paclitaxel-resistant HCT-15 human colorectal cancer cells.

Source: Rexahn Pharmaceuticals