1. Synthesis of minoxidil conjugates and their evaluation as HL-60 differentiation agents.
- Author
-
Stoica S, Magoulas GE, Antoniou AI, Suleiman S, Cassar A, Gatt L, Papaioannou D, Athanassopoulos CM, and Schembri-Wismayer P
- Subjects
- Aniline Compounds chemistry, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Cell Differentiation drug effects, Cell Proliferation drug effects, Fluorenes chemistry, HL-60 Cells, Humans, Imidazoles chemistry, Polyamines chemistry, Spermine chemistry, Antineoplastic Agents chemical synthesis, Minoxidil chemistry
- 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., (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Published
- 2016
- Full Text
- View/download PDF