Diversity oriented synthesis and IKK inhibition of aminobenzimidazole tethered quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines.

Abstract:

:The derivatization of resin-bound aminobenzimidazole toward the parallel solid-phase synthesis of aminobenzimidazole tethered pharmacologically important heterocycles such as quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines is reported. All the compounds were tested for IKK inhibition. Only one compound elicited significant inhibition of IKKε, TBK-1 and IKK2.

journal_name

Bioorg Med Chem Lett

authors

Dadiboyena S,Arfaoui A,Amri H,Piedrafita FJ,Nefzi A

doi

10.1016/j.bmcl.2014.11.078

subject

Has Abstract

pub_date

2015-02-01 00:00:00

pages

685-9

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01285-2

journal_volume

25

pub_type

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