7107-59-7Relevant articles and documents
Positioning of an unprecedented 1,5-oxaza spiroquinone scaffold into SMYD2 inhibitors in epigenetic space
Dhorma, Lama Prema,Kim, Mi-hyun,Maeng, Han-Joo,Maturi, Arunkranthi,Mirzaei, Anvar,Nangunuri, Bhargav Gupta,Ragam, Rao,Teli, Mahesh K.,Venkanna, Arramshetti,Vo, Dang-Khoa
supporting information, (2021/10/16)
Lysine methyltransferases are important regulators of epigenetic signaling and are emerging as a novel drug target for drug discovery. This work demonstrates the positioning of novel 1,5-oxaza spiroquinone scaffold into selective SET and MYND domain-conta
One stone two birds: Cobalt-catalyzed in situ generation of isocyanates and benzyl alcohols for the synthesis of N-aryl carbamates
Li, Sida,Khan, Ruhima,Zhang, Xia,Yang, Yong,Wang, Zheting,Zhan, Yong,Dai, Yuze,Liu, Yue-E,Fan, Baomin
, p. 5891 - 5896 (2019/06/24)
An efficient method for the synthesis of N-aryl carbamates from N-Boc-protected amines has been developed. The cobalt-catalyzed in situ generation of isocyanates from N-Boc-protected amines and benzyl alcohols from benzyl formates has been achieved for the first time, which in turn furnished the corresponding benzyl carbamates in moderate to high yields. The reaction was catalyzed by CoI2 with tris-(4-dimethylaminophenyl)-phosphine as the ligand and zinc powder as the reductant. The developed reaction conditions were found to be compatible for aromatic amines with both electron-donating and -withdrawing substituents.
Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane x receptor antagonists
Hodnik, ?iga,Peterlin Ma?i?, Lucija,Toma?i?, Tihomir,Smodi?, Domen,D'Amore, Claudio,Fiorucci, Stefano,Kikelj, Danijel
, p. 4819 - 4833 (2014/07/07)
Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts as a xenobiotic sensor and a paramount transcriptional regulator of drug-metabolizing enzymes and transporters. The overexpression of PXR in various cancer cells indicates the importance of PXR as a drug target for countering multidrug resistance in anticancer treatments. We describe the discovery of novel bazedoxifene-scaffold-based PXR antagonists inspired by the marine sulfated steroids solomonsterol A and B as natural leads. A luciferase reporter assay on a PXR-transfected HepG2 cell line identified compounds 19-24 as promising PXR antagonists. Further structure-activity relationship studies of the most active PXR antagonist from the series (compound 20, IC50 = 11 μM) revealed the importance of hydroxyl groups as hydrogen-bond donors for PXR antagonistic activity. PXR antagonists 20 and 24 (IC50 = 14 μM), in addition to the downregulation of PXR expression, exhibited inhibition of PXR-induced CYP3A4 expression, which illustrates their potential to suppress PXR-regulated phase-I drug metabolism.