March 24, 2017
This invention relates to novel anti-cancer compounds consisting of rhenium which are (i) more potent than platinum-based chemotherapeutic agents such as cisplatin and (ii) show anti-cancer activity against cisplatin-resistant cancer cells.
About half of treated cancer patients receive platinum-based drugs (eg. cisplatin, carboplatin) alone or in co-administration with other anticancer agents. Despite their efficacy, their use is limited by toxic side effects and inherent or acquired resistance to platinum-based drugs by tumor cells.
The present rhenium (I) complexes contain axial water ligands for enhanced water solubility to enable better formulation. In addition, the lead complex shows increased potency both in non-resistant and cisplatin-resistant tumor cells.
Table 1 . Anticancer activities in human cervical cancer cells (HeLa)
Table 2 . Anticancer activities in Chemo-sensitive and Chemo-resistant cancer cell lines
Treatment of cisplatin-resistant tumors.
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anti-cancer compounds consisting
show anti-cancer activity
toxic side effects
axial water ligands
enhanced water solubility
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