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 a research article in Bioorganic & Medicinal Chemistry [18:7966-7974, 2010] on the anticancer activity of quinoxalinyl-piperazine compounds.
“The quinoxalinyl-piperazine compounds are a new chemical entity that exhibits potent anticancer properties”
The study demonstrates that the quinoxalinyl-piperazine compounds strongly inhibit the growth of human cancer cells through programmed cell death (apoptosis), including paclitaxel (Taxol®) resistant HCT-15 human colorectal cancer cells. Those compounds also display the synergistic cytotoxic effect when combined with several known cancer drugs such as paclitaxel, doxorubicin, cisplatin, gemcitabine or 5-fluorouracil in cancer cells.
For example, using HCT116 and paclitaxel resistant HCT-15 cancer cells, a compound showed the same potent inhibitory effect in both cancer cells. But the compound had an even stronger effect in drug resistant HCT-15 cells compared to the anticancer activity of paclitaxel, decreasing cancer growth by 70-fold in paclitaxel resistant HCT-15 cells. This result implies that the compound may control and overcome drug resistance.
"The quinoxalinyl-piperazine compounds are a new chemical entity that exhibits potent anticancer properties," said Rick Soni, President of Rexahn, "In addition, the current study clearly demonstrates that these compounds significantly inhibited growth of both human cancer cells and drug-resistant cancer cells and have potential use in combination therapy with other clinically approved anticancer drugs to provide stronger, less toxic therapies."
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