5488-36-8Relevant articles and documents
1,3,4-OXADIAZOLE HOMOPHTHALIMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
Page/Page column 102-103, (2020/12/11)
The present invention relates to novel compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a medicinal use thereof, and a method for preparing the same. The novel compounds according to the present invention, stereoisomers thereof or pharmaceutically acceptable salts thereof have the histone deacetylase 6 (HDAC6) inhibitory activity, and are effective in preventing or treating HDAC6-related diseases, comprising infectious diseases; neoplasm; endocrinopathy; nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; eye and ocular adnexal diseases; circulatory diseases; respiratory diseases; digestive diseases; skin and subcutaneous tissue diseases; musculoskeletal system and connective tissue diseases; and teratosis or deformities, or chromosomal aberration.
Intramolecular photoreactions of thiohomophthalimides with an alkenyl group in their N-side chain. Regioselective synthesis of heterocycle-fused isoquinoline derivatives through [2+2] photocycloaddition
Takechi, Haruko,Takahashi, Hajime,Machida, Minoru
, p. 201 - 207 (2007/10/03)
Upon irradiation, thiohomophthalimides with an alkenyl group in their N-side chain or at the benzylic position give tricyclic isoquinoline derivatives through regioselective intramolecular [2+2] cycloaddition or Norrish type II reaction, respectively, in
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A new class of inhibitors of lck kinase
Snow, Roger J.,Cardozo, Mario G.,Morwick, Tina M.,Busacca, Carl A.,Dong, Yong,Eckner, Robert J.,Jacober, Stephen,Jakes, Scott,Kapadia, Suresh,Lukas, Susan,Panzenbeck, Maret,Peet, Gregory W.,Peterson, Jeffrey D.,Prokopowicz III, Anthony S.,Sellati, Rosemarie,Tolbert, Robert M.,Tschantz, Matt A.,Moss, Neil
, p. 3394 - 3405 (2007/10/03)
An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5′-triphosphate competitive inhibitor of lck by high throughput screening. Initial structure-activity relationship studies identified the dichlorophenyl ring and the imide NH as important pharmacophores. A binding model was constructed to understand how 1 binds to a related kinase, hck. These results suggested that removing the gem-dimethyl group and flattening the ring would enhance activity. This was realized by converting 1 to the imidazo[4,5-h]isoquinolin-9-one (20), resulting in an 18-fold improvement in potency against lck and a 50-fold increase in potency in a cellular assay.