1036204-60-0Relevant articles and documents
Assembly of [2]Rotaxanes in Water
Aeschi, Yves,Drayss-Orth, Sylvie,Valá?ek, Michal,Raps, Felix,H?ussinger, Daniel,Mayor, Marcel
, p. 4091 - 4103 (2017)
Two [2]rotaxanes have been assembled in water from modular subunits through CuI-catalyzed azide–alkyne “click” chemistry. For this purpose, 2,6-disubstituted naphthalene axles with solubilizing oligo(ethylene glycol) (OEG) chains (n = 1–5) and propargyl terminal groups were synthesized and examined for their propensity to form inclusion complexes with a dicationic Diederich-type cyclophane host. The dependence of pseudorotaxane formation on the linkers between the naphthalene core and OEG chains, and in the case of ester linkers on different spacer lengths, was analyzed by titration experiments. In addition, the inclusion complexes of two [2]rotaxanes were trapped by using a water-soluble azide-functionalized stopper. Repetitive chromatography finally enabled the isolation of both mechanically interlocked [2]rotaxanes.
The design, synthesis and anti-tumor mechanism study of new androgen receptor degrader
Xie, Hang,Liang, Jian-Jia,Wang, Ya-Lei,Hu, Tian-Xing,Wang, Jin-Yi,Yang, Rui-Hua,Yan, Jun-Ke,Zhang, Qiu-Rong,Xu, Xia,Liu, Hong-Min,Ke, Yu
, (2020/07/31)
Targeted protein degradation using small molecules is a novel strategy for drug development. In order to solve the problem of drug resistance in the treatment of prostate cancer, proteolysis-targeting chimeras (PROTAC) was introduced into the design of anti-prostate cancer derivatives. In this work, we synthesized two series of selective androgen receptor degraders (SARDs) containing the hydrophobic degrons with different linker, and then investigated the structure-activity relationships of these hybrid compounds. Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Among them, compound A9 displayed potent inhibitory activity against LNCaP prostate cancer cell line with IC50 values of 1.75 μM, as well as excellent AR degradation activity. Primary mechanism studies elucidated compound A9 arrested cell cycle at G0/G1 phase and induced a mild apoptotic response in LNCaP cells. Further study indicated that the degradation of AR was mediated through proteasome-mediated process. For all these reasons, compound A9 held promising potential as anti-proliferative agent for the development of highly efficient SARDs for drug-resistance prostate cancer therapies.
Compounds and methods for inhibiting phosphate transport
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Page/Page column 562, (2016/05/02)
Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
