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Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents

E Yee, E Pasquier, G Iskander, K Wood D Stc Black and N Kumar from the a School of Chemistry, the Children’s Cancer Institute Australia for Medical Research, Lowy Cancer Research Centre, University of NSW, Randwick, and the Metronomics Global Health Initiative have just reported in Bioorganic & Medicinal Chemistry an article entitled : Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents

They report that Isoflavene-propranolol hybrid molecules developed as potentially novel anti-tumour agents. These hybrids might be highly valuable since Isoflavene itself has potent anti-cancer activity while propranolol can enhance anti-proliferative and anti-angiogenic properties of 5-fluorouracil and paclitaxel. These analogues were tested in anti-cancer cell viability assays against SHEP neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines, and were found to exhibit potent anti-proliferative activities. These compounds also displayed anti-angiogenic and anti-proliferative effects in HMEC-1 human microvascular endothelial cell lines. Of note, the most potent synthesized hybrids displayed enhanced potency against cancer cell lines compared to either isoflavene or propranolol alone.