2. Academic Validation
  3. Synthesis of minoxidil conjugates and their evaluation as HL-60 differentiation agents

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

  • Bioorg Med Chem Lett. 2016 Feb 15;26(4):1145-50. doi: 10.1016/j.bmcl.2016.01.048.
Sonia Stoica 1,  George E Magoulas 2,  Antonia I Antoniou 2,  Sherif Suleiman 1,  Analisse Cassar 1,  Lucienne Gatt 1,  Dionissios Papaioannou 2,  Constantinos M Athanassopoulos 3,  Pierre Schembri-Wismayer 4
Affiliations

Affiliations

  • 1 Anatomy Department, Faculty of Medicine and Surgery, University of Malta, Malta.
  • 2 Laboratory of Synthetic Organic Chemistry, Department of Chemistry, University of Patras, GR-26504 Patras, Greece.
  • 3 Laboratory of Synthetic Organic Chemistry, Department of Chemistry, University of Patras, GR-26504 Patras, Greece. Electronic address: kath@chemistry.upatras.gr.
  • 4 Anatomy Department, Faculty of Medicine and Surgery, University of Malta, Malta. Electronic address: pierre.schembri-wismayer@um.edu.mt.
PMID: 26832215 DOI: 10.1016/j.bmcl.2016.01.048
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.

Keywords

Conjugates; Differentiation; HL-60; Minoxidil; Polyamines.

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