153826-05-2Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of benzodiazepine-based SUMO-specific protease 1 inhibitors
Qiao, Zhitao,Wang, Weiwei,Wang, Lie,Wen, Donghua,Zhao, Yaxue,Wang, Qing,Meng, Qingqing,Chen, Guoqiang,Wu, Yingli,Zhou, Huchen
, p. 6389 - 6392 (2011/11/29)
As the best-characterized ubiquitin-like protein (UBL), small ubiquitin-related modifier (SUMO) was found to conjugate with a number of proteins to regulate cellular functions including transcription, signal transduction, and cell cycle. While E1, E2 and E3 ligases are responsible for the forward SUMOylation reaction, SUMO-specific proteases (SENPs) reversibly removeSUMOfrom the SUMOylated proteins. Recently, SENP1 was found to be a potential therapeutic target for the treatment of prostate cancers, but the design and synthesis of its inhibitors have not been reported. We designed and synthesized a series of benzodiazepinebased SENP1 inhibitors, and they showed inhibitory activity as good as IC50 = 9.2 μM (compound 38). The structure-activity relationship was also discussed.
Development of 1,4-Benzodiazepine Cholecystokinin Type B Antagonists
Bock, Mark G.,DiPardo, Robert M.,Evans, Ben E.,Rittle, Kenneth E.,Whitter, Willie L.,et al.
, p. 4276 - 4292 (2007/10/02)
A series of 3-(arylureido)-5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin (CCK), are described.Derived by reasoned modification of the CCK-A selective 3-carboxamido-1,4-benzodiazepine, MK-329, this paper chronicles the development of potent, orally effective compounds in which selectivity for the CCK-B recebtor subtype was achieved.The principal lead structure that emerged from these studied is L-365,260, a compound which has been submitted for clinical evaluation.Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK-B receptor affinity and selectivity of this class of compounds.
