Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2)
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.
Playa, Hilaire,Lewis, Timothy A.,Ting, Amal,Suh, Byung-Chul,Muoz, Benito,Matuza, Robert,Passer, Brent J.,Schreiber, Stuart L.,Buolamwini, John K.
supporting information
p. 5801 - 5804
(2015/01/08)
An alternative oxidising and brominating method converting alcohols to aldehydes and β-bromoethyl esters using ionic liquid [Bmim][Br3]
[Bmim][Br3] is an oxidising reagent which converts alcohols into aldehydes and ketones in mild conditions and good yields; the use of the ionic liquid (IL) as both an oxidising and a brominating reagent in the one-pot synthesis of β-bromoethyl esters from benzyl alcohols and diols has also been studied.
Zhang, Yu,Bao, Weiliang
p. 263 - 266
(2007/10/03)
One-pot synthesis of ω-bromoesters from aromatic aldehydes and diols using pyridinium hydrobromide perbromide
A simple and efficient one-pot procedure has been developed for the synthesis of ω-bromoesters from aromatic aldehydes and diols in the presence of pyridinium hydrobromide perbromide (PHPB) and triethoxymethane in which aldehyde reacts first with diol and the product, cyclic acetal, reacts with PHPB to give the final product, ω-bromoesters.
Aoyama, Tadashi,Takido, Toshio,Kodomari, Mitsuo
p. 1989 - 1992
(2007/10/03)
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