Synthesis of Minoxidil Conjugates and Their Evaluation as HL-60 Differentiation Agents

January 2016 in “ Bioorganic & Medicinal Chemistry Letters ”

Sonia Stoica, George E. Magoulas, Antonia I. Antoniou, Sherif Suleiman, Analisse Cassar, Lucienne Gatt, Dionissios Papaioannou, Constantinos M. Athanassopoulos, Pierre Schembri-Wismayer

minoxidil MNX HL-60 spermine SPM 4,4'-methylenedianiline MDA 2,7-diaminofluorene DAF polyamines amines Rogaine

TLDR Some minoxidil combinations can help differentiate leukemia cells without harming other cells.

In the 2016 study by Stoica et al., researchers synthesized minoxidil (MNX) conjugates to assess their ability to induce differentiation in HL-60 acute myeloid leukemia cells. The conjugates were created by combining MNX with natural polyamines and various amines. The study revealed that MNX alone did not induce differentiation, but specific conjugates, particularly the MNX-spermine (SPM) conjugate (11) and conjugates 7 and 8 with 4,4'-methylenedianiline (MDA) and 2,7-diaminofluorene (DAF), did show differentiation effects at 10 µM concentration without being toxic to proliferating human peripheral blood mononuclear cells. These findings suggest that MNX conjugation with certain amines can enhance its biological activity and could provide a targeted approach to leukemia treatment with reduced cytotoxicity. Further research is needed to expand the library of MNX-amine and -polyamine conjugates and to understand the mechanisms behind the differentiation induction.

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Synthesis of Minoxidil Conjugates and Their Evaluation as HL-60 Differentiation Agents

Research cited in this study

research Minoxidil Upregulates the Expression of Vascular Endothelial Growth Factor in Human Hair Dermal Papilla Cells

research Biphasic Effects of Minoxidil on the Proliferation and Differentiation of Normal Human Keratinocytes

research Suppression of Fibroblast Proliferation and Lysyl Hydroxylase Activity by Minoxidil

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