Glioblastoma Multiforme (GBM) is the most common and deadliest of malignant primary brain tumors in adults. In the United States, approximately 20,000 patients are diagnosed with GBM each yearand the mean life expectancy of these patients is approximately one year. Among the recent clinical therapy approaches, only the combined therapy of Temozolomide and radiation treatment produced encouraging clinical results in long term survival of patients. Therefore, there is a substantial need for the development of new and more effective chemotherapeutic agents to treat GBM.  In continuation of our effort to identify new anti-glioma agents, we synthesized a novel 1,2,3,4-Tetrahydroisoquinoline ( EDL-155)  analogs and screened them for their anti-glioma activity in four established human glioma cell lines (T98, U87, LN18 and A172).  We discovered the EDL-358  as a potent and selective anti-glioma agent (A172 IC50: 8.25 �0.42 �M), which displayed a similar cytotoxicity profile as standard Temozolamide in human glioma cell lines.

Synthesis and in vitro evaluation of novel 1,2,3,4-tetrahydroisoquinoline derivatives as potent anti-glioma agents

246th National Meeting (2013)

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