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Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).


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.

SUBMITTER: Playa H 

PROVIDER: S-EPMC5695681 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature

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Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).

Playa Hilaire H   Lewis Timothy A TA   Ting Amal A   Suh Byung-Chul BC   Muñoz Benito B   Matuza Robert R   Passer Brent J BJ   Schreiber Stuart L SL   Buolamwini John K JK  

Bioorganic & medicinal chemistry letters 20141028 24


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 inhi  ...[more]

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