期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 4, 页码 1145-1150出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.01.048
关键词
Minoxidil; Conjugates; Polyamines; Differentiation; HL-60
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 mu M without being toxic on proliferating human peripheral blood mononuclear cells. (C) 2016 Elsevier Ltd. All rights reserved.
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