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

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• 作者：Sonia Stoica^a ; George E. Magoulas^b ; Antonia I. Antoniou^b ; Sherif Suleiman^a ; Analisse Cassar^a ; Lucienne Gatt^a ; Dionissios Papaioannou^b ; Constantinos M. Athanassopoulos^b ; ^{kath@chemistry.upatras.gr" class="auth_mail" title="E-mail the corresponding author} ; Pierre Schembri-Wismayer^a ; ^{pierre.schembri-wismayer@um.edu.mt" class="auth_mail" title="E-mail the corresponding author}
• 关键词：DTHRTNXFSCFNOM-UHFFFAOYSA-N ; PPQSFZRSLJJGIO-UHFFFAOYSA-N ; KTBLWQMXNNJJDB-UHFFFAOYSA-N ; WPIVUAYYIHTPHF-UHFFFAOYSA-N ; DIEPVYVXKTWHOY-UHFFFAOYSA-N ; GUWQCSZWDGEKSN-UHFFFAOYSA-N ; FLMOMRLVPYSISM-UHFFFAOYSA-N ; DLAIMBUGPMGORD-UHFFFAOYSA-N ; VFUXZZSUIQDJME-UHFFFAOYSA-N ; ZFMITUMMTDLWHR-UHFFFAOYSA-N
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：26
• 期：4
• 页码：1145-1150
• 全文大小：1893 K

文摘

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.