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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Dadiboyena, Sureshbabu¹  Arfaoui, Aicha²  Amri, Hassen²  Piedrafita, F. Javier³  Nefzi, Adel¹ 

[1] Torrey Pines Inst Mol Studies, Port St Lucie, FL 34987 USA

[2] Univ El Manar, Fac Sci Tunis, Lab Select Organ Chem & Biol Act, El Manar 2092, Tunisia

[3] Torrey Pines Inst Mol Studies, San Diego, CA 92121 USA

关键词: Solid-phase synthesis;    Aminobenzimidazoles;    Quinazolinediones;    Thioxoquina-zolinones;    Benzodiazepinetriones;    Intramolecular cyclization;    Isoxazoles;    Isoxazolines;    1,3-Dipolar cycloaddition;    Heterocycles;   

DOI  :  10.1016/j.bmcl.2014.11.078

来源: Elsevier

【 摘 要 】

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 IKK epsilon, TBK-1 and IKK2. (C) 2014 Elsevier Ltd. All rights reserved.

【 授权许可】

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