104004-96-8Relevant articles and documents
Photorearrangement of Quinoline-Protected Dialkylanilines and the Photorelease of Aniline-Containing Biological Effectors
Deodato, Davide,Asad, Naeem,Dore, Timothy M.
, p. 7342 - 7353 (2019)
The direct release of dialkylanilines was achieved by controlling the outcome of a photorearrangement reaction promoted by the (8-cyano-7-hydroxyquinolin-2-yl)methyl (CyHQ) photoremovable protecting group. The substrate scope was investigated to obtain structure-activity relationships and to propose a reaction mechanism. Introducing a methyl substituent at the 2-methyl position of the CyHQ core enabled the bypass of the photorearrangement and significantly improved the aniline release efficiency. We successfully applied the strategy to the photoactivation of mifepristone (RU-486), an antiprogestin drug that is also used to induce the LexPR gene expression system in zebrafish and the gene-switch regulatory system based on the pGL-VP chimeric regulator in mammals.
Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer
Lin, Yuqi,Liu, Rong,Zhao, Ping,Ye, Jinxiang,Zheng, Zheng,Huang, Jingan,Zhang, Yingying,Gao, Yu,Chen, Haiying,Liu, Suling,Zhou, Jia,Chen, Ceshi,Chen, Haijun
, p. 354 - 367 (2018)
Triple-negative breast cancer (TNBC) is one of the most malignant breast cancers currently with a lack of targeted therapeutic drugs. Accumulating evidence supports that KLF5 represents a novel therapeutic target for the treatment of basal TNBC. Our previ
ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
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Page/Page column 129-130, (2021/05/21)
The disclosure relates to anti-cancer compounds which are anti-cancer PARP inhibitors of formula Al, A2, A3 or A4 conjugated by a linker to a steroid, whereby the steroid targets the conjugate to the nucleus, as well as to methods for their preparation and use. (I)
