Synthesis of minoxidil conjugates and their evaluation as HL-60 differentiation agents

Bioorganic & Medicinal Chemistry Letters
Sonia StoicaPierre Schembri-Wismayer

Abstract

Activation of minoxidil (MNX) with N,N'-carbonyldiimidazole and coupling with natural polyamines (PAs) and commercially available aliphatic or aromatic amines provided a series of new conjugates which were evaluated for their ability to induce differentiation to HL-60 acute myeloid leukemia cancer cells, using a modified NBTZ reduction test. Although neither MNX nor 4,4'-methylenedianiline (MDA) or 2,7-diaminofluorene (DAF), alone or in combination, had any effect, the MNX-spermine (SPM) conjugate (11) and the conjugates 7 and 8 of MNX with MDA and DAF exhibited a differentiation-inducing effect at a concentration of 10 μM without being toxic on proliferating human peripheral blood mononuclear cells.

References

Feb 26, 2011·International Journal of Cancer. Journal International Du Cancer·Jacques FerlayDonald Maxwell Parkin
May 14, 2014·Drug Discovery Today·Panagiota A SotiropoulouDaniele Passarella
Dec 10, 2014·Clinical Lymphoma, Myeloma & Leukemia·Elihu H Estey

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Citations

Dec 17, 2016·The Journal of Pharmacology and Experimental Therapeutics·Terry PetrouAamir Ahmed
Oct 25, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Despina PallaConstantinos M Athanassopoulos

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