54256-43-8Relevant articles and documents
Nonpeptidic, Polo-Box Domain-Targeted Inhibitors of PLK1 Block Kinase Activity, Induce Its Degradation and Target-Resistant Cells
Chapagai, Danda,Ramamoorthy, Gurusankar,Varghese, Jessy,Nurmemmedov, Elmar,McInnes, Campbell,Wyatt, Michael D.
supporting information, p. 9916 - 9925 (2021/07/26)
PLK1, polo-like kinase 1, is a central player regulating mitosis. Inhibition of the subcellular localization and kinase activity of PLK1 through the PBD, polo-box domain, is a viable alternative to ATP-competitive inhibitors, for which the development of resistance and inhibition of related PLK family members are concerns. We describe novel nonpeptidic PBD-binding inhibitors, termed abbapolins, identified through successful application of the REPLACE strategy and demonstrate their potent antiproliferative activity in prostate tumors and other cell lines. Furthermore, abbapolins show PLK1-specific binding and inhibitory activity, as measured by a cellular thermal shift assay and an ability to block phosphorylation of TCTP, a validated target of PLK1-mediated kinase activity. Additional evidence for engagement of PLK1 was obtained through the unique observation that abbapolins induce PLK1 degradation in a manner that closely matches antiproliferative activity. Moreover, abbapolins demonstrate antiproliferative activity in cells that are dramatically resistant to ATP-competitive PLK1 inhibitors.
Preparation of new substituted bis(benzoyl) peroxides under aqueous conditions in the presence of stearyltrimethylammonium chloride
Moorhoff, Cornelis M.,Braybrook, Carl
, p. 397 - 405 (2007/10/03)
A series of new substituted bis(benzoyl) peroxides has been synthesised from their corresponding acid chlorides in high yield. The reactions were carried out in aqueous sodium peroxide solution and butanone in the presence of 0.5% stearyltrimethylammonium chloride (STAC) at a temperature below 15°C. STAC improved the purity, and the fast addition improved the yield of the peroxides. Mass spectral analysis of substituted bis(benzoyl) peroxides using EI has been carried out for accurate mass determinations. Springer-Verlag 2003.
Mesomorphic Properties of Some 4,4'-Alkyl and Alkoxy Disubstituted Phenylbenzoates
Neubert, Mary E.,Jirousek, Michael R.,Hanlon, Carol A.
, p. 223 - 234 (2007/10/02)
A variety of new 4,4'-disubstituted phenylbenzoates with one and/or both substituents as alkyl (R) or alkoxy (RO) were prepared and their mesomorphic (liquid crystalline) properties determined for later use as standards for comparison with mesomorphic properties in other new 4,4'-disubstituted phenylbenzoates.Other esters of this type which had been previously reported, were prepared for physical studies of their mesophases and found to have different mesomorphic properties than those reported earlier.Still others were prepared to identify phases which were not determined previously.This paper presents new mesomorphic properties along with a comparison of the NMR spectra for the four possible analogs of these esters (R-R, R-OR), RO-R, RO-OR).Keywords: phenylbenzoates, mesogens, liquid crystals, NMR