Synthesis of isoflavene-thiosemicarbazone hybrids and evaluation of their anti-tumor activity |
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| Authors: | Eugene MH Yee Miriam B Brandl David StC Black Orazio Vittorio Naresh Kumar |
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| Institution: | 1. School of Chemistry, The University of New South Wales, Sydney, NSW 2052, Australia;2. Children’s Cancer Institute Australia, Lowy Cancer Research Centre, UNSW, Randwick, NSW, Australia;3. Australian Centre for NanoMedicine, University of New South Wales, Sydney, NSW 2052, Australia |
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| Abstract: | Phenoxodiol is an isoflavene with potent anti-tumor activity. In this study, a series of novel mono- and di-substituted phenoxodiol-thiosemicarbazone hybrids were synthesized via the condensation reaction between phenoxodiol with thiosemicarbazides. The in vitro anti-proliferative activities of the hybrids were evaluated against the neuroblastoma SKN-BE(2)C, the triple negative breast cancer MDA-MB-231, and the glioblastoma U87 cancer cell lines. The mono-substituted hybrids exhibited potent anti-proliferative activity against all three cancer cell lines, while the di-substituted hybrids were less active. Selected mono-substituted hybrids were further investigated for their cytotoxicity against normal MRC-5 human lung fibroblast cells, which identified two hybrids with superior selectivity for cancer cells over normal cells as compared to phenoxodiol. This suggests that mono-substituted phenoxodiol-thiosemicarbazone hybrids have promising potential for further development as anti-cancer agents. |
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| Keywords: | Isoflavene Phenoxodiol Anti-cancer Thiosemicarbazone |
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