Bifidenone is a novel natural tubulin polymerization inhibitor that exhibits antiproliferative activity against a range of human cancer cell lines. To that end, over 300 analogues were synthesized to examine the structure-activity relationship of bifidenone derivatives.  Among those analogues, SQ1274 has been selected to a preclinical candidate based on efficacy in murine xenograft experiments. Here, a synthetic method of SQ1274 is described. The absolute stereochemistry of SQ1274 is determined by single crystal X-ray analysis.

Preparation of a preclinical candidate SQ1274

256th National Meeting (2018)

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