Survival rate of acute myeloid leukemia (AML) is still poor underscoring the need for innovative treatments with novel mechanisms of action. To this end, we have regioselectively synthesized dimeric naphthoquinone (BiQ) analogues possessing anti-AML activity. Here, we report the rational design and synthesis of a series of BiQs that contain aminohydroxyl moiety on one or both naphthoquinone cores. These compounds, compared with the first and second generation BiQs, have superior chemical stability, improved aqueous solubility and are more potent (nanomolar range) against AML cells particularly the cells with FLT3-ITD mutations. In this poster, structure activity studies, solubility and metabolic stability data of lead compounds will be presented.

Rational design and synthesis of potent and aqueous soluble bis-amino alcohol dimeric naphthoquinones with activity against acute myeloid leukemia cells

255th National Meeting (2018)

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