期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 24, 页码 5801-5804出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.026
关键词
Equilibrative nucleoside transporters (ENTs); hENT1; hENT2; rENT2; Dilazep
资金
- NIH-MLPCN program [1 U54 HG005032-1]
- NIH [RO1GM10405, RO1CA102139]
As ENT inhibitors including dilazep have shown efficacy improving oHSV1 targeted oncolytic cancer therapy, a series of dilazep analogues was synthesized and biologically evaluated to examine both ENT1 and ENT2 inhibition. The central diamine core, alkyl chains, ester linkage and substituents on the phenyl ring were all varied. Compounds were screened against ENT1 and ENT2 using a radio-ligand cell-based assay. Dilazep and analogues with minor structural changes are potent and selective ENT1 inhibitors. No selective ENT2 inhibitors were found, although some analogues were more potent against ENT2 than the parent dilazep. (C) 2014 Elsevier Ltd. All rights reserved.
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