CXCR4 is the most common chemokine receptor expressed on the surface of many cancer cell types. In comparison to normal tissues, CXCR4 is overexpressed by cancer cells and correlates with cancer cell metastasis, angiogenesis and tumor growth. CXCR4 antagonists can potentially diminish the viability of cancer cells by interfering with CXCL12-mediated pro-survival signaling and by inhibiting chemotaxis. Over the last several years some academic groups and companies have developed small molecule CXCR4 antagonists that are being investigated as potential cancer therapeutics. Our group has discovered a series of novel tetrahydroisoquinoline based small molecules that are potent CXCR4 antagonists. Herein is presented recent structure-activity studies to improve upon target specificity and metabolic stability.

Synthesis and SAR of TIQ-15 based CXCR4 antagonists: Identification of tetrahydroquinoline replacements

253rd National Meeting (2017)

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