Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).
Bioorg Med Chem Lett
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Abstract | 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. |
Year of Publication | 2014
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Journal | Bioorg Med Chem Lett
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Volume | 24
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Issue | 24
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Pages | 5801-4
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Date Published | 2014 Dec 15
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ISSN | 1464-3405
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DOI | 10.1016/j.bmcl.2014.10.026
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PubMed ID | 25454272
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Grant list | R01 GM104503 / GM / NIGMS NIH HHS / United States
1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States
R01CA102139 / CA / NCI NIH HHS / United States
R01GM10405 / GM / NIGMS NIH HHS / United States
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