Authors Bueno, O; Gargantilla, M; Estevez-Gallego, J; Martins, S; Diaz, JF; Camarasa, MJ; Liekens, S; Perez-Perez, MJ; Priego, EM in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about VASCULAR DISRUPTING AGENTS; INHIBITORS; COMPLEX; DESIGN in [Bueno, Oskia; Gargantilla, Marta; Jose Camarasa, Maria; Perez-Perez, Maria-Jesus; Priego, Eva-Maria] CSIC, IQM, Juan Cierva 3, Madrid 28006, Spain; [Estevez-Gallego, Juan; Fernando Diaz, J.] CSIC, CIB, Ramiro Maeztu 9, Madrid 28040, Spain; [Martins, Solange; Liekens, Sandra] Katholieke Univ Leuven, Rega Inst Med Res, Herestr 49, B-3000 Leuven, Belgium in 2019.0, Cited 39.0. Product Details of 101-84-8. The Name is Diphenyl oxide. Through research, I have a further understanding and discovery of 101-84-8
Microtubule targeting agents represent a very active arena in the development of anticancer agents. In particular, compounds binding at the colchicine site in tubulin are being deeply studied, and the structural information recently available on this binding site allows structure-directed design of new ligands. Structural comparison of our recently reported high resolution X-Ray structure of the cyclohexanedione derivative TUB075 bound to tubulin and the tubulin-DAMA-colchicine complex has revealed a conformational change in the alpha T5 loop. By a grid-based computational analysis of the tubulin-DAMA-colchicine binding site, we have identified a new favourable binding area in the colchicine-site that was unexplored by our lead TUB075. Thus, based on a structure-guided design, new cyclohexanedione derivatives have been synthesized and tested for tubulin binding and in cellular assays. As a result, we have identified diphenyl ether derivatives with IC50 values around 10-40 nM against three different tumor cell lines and affinity constants for tubulin similar to that of colchicine around 10(7) M-1. As expected, they halted the cell cycle progression at G2/M phase at concentrations as low as 0.08 mu M. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Ether – Wikipedia,
,Ether | (C2H5)2O – PubChem