1080643-87-3Relevant academic research and scientific papers
Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure-Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1
Hansen, Joshua D.,Condroski, Kevin,Correa, Matthew,Muller, George,Man, Hon-Wah,Ruchelman, Alexander,Zhang, Weihong,Vocanson, Fan,Crea, Tim,Liu, Wei,Lu, Gang,Baculi, Frans,Lebrun, Laurie,Mahmoudi, Afshin,Carmel, Gilles,Hickman, Matt,Lu, Chin-Chun
, p. 492 - 503 (2018/02/07)
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure-activity relationships for analogs of 3 with exploration of the structurally related dioxoisoindoline class. The observed activity of protein degradation could in part be rationalized through docking into the previously disclosed 3-CRBN-GSPT1 cocrystal ternary complex. For SAR that could not be rationalized through the cocrystal complex, we sought to predict SAR through a QSAR model developed in house. Through these analyses, selective protein degradation could be achieved between the two proteins of interest, GSPT1 and Aiolos.
Aniline carbamates: A versatile and removable motif for palladium-catalyzed directed c-h activation
Uhlig, Nick,Li, Chao-Jun
, p. 12066 - 12070 (2015/03/31)
The aniline carbamate is introduced as a new removable directing group for C-H activation. Its versatility and ability as a directing group are demonstrated by its use in the ortho-arylation of a wide variety of aniline derivatives under palladium(II) catalysis, with symmetric diaryliodonium salts as aryl donors. The reaction differs from previously reported arylations in its selectivity and its mechanism, as elucidated by kinetic and isotopic experiments. The directing group can also be easily removed under a variety of conditions.
Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists
Sakamoto, Toshihiro,Moriya, Minoru,Haga, Yuji,Takahashi, Toshiyuki,Shibata, Takunobu,Okamoto, Osamu,Nonoshita, Katsumasa,Kitazawa, Hidefumi,Hidaka, Masayasu,Gomori, Akira,Iwaasa, Hisashi,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro,Gao, Ying-Duo,MacNeil, Douglas J.,Yang, Lihu
scheme or table, p. 1564 - 1568 (2009/12/07)
A series of spiroindoline-3,4′-piperidine derivatives were synthesized and evaluated for their binding affinities and antagonistic activities at Y5 receptors. Potent Y5 antagonists were tested for their oral bioavailabilities and brain penetration in rats
