Multidrug resistance (MDR) is a phenomenon in which administration of a single chemotherapeutic agent can cause cross-resistance to a variety of other therapies. Development of MDR against current therapies is a major challenge in the treatment of cancer. Previously, we have demonstrated the ability of sHA 14-1 to mitigate drug resistance and synergize with a variety of chemotherapeutic agents. This presentation will describe a thorough structure-activity relationship study of sHA 14-1 leading to the identification of CXL017, which is 23-fold more potent than sHA 14-1. CXL017 can selectively target MDR cell lines cross-resistant to a variety of known chemotherapeutic agents in vitro. In addition, CXL017 shows significant anti-tumor acitivity against drug resistant tumors in vivo. Importantly, MDR cell lines continously treated with CXL017 over a period of six months fail to develop resistance. These results suggest that CXL017 is a promising candidate for treatment of cancer with MDR.

Synthesis of anticancer agents that selectively target drug resistant cancer

241st National Meeting (2011)

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