Ruthenium-containing P450 inhibitors for dual enzyme inhibition and DNA damage
Cytochrome P450s are key players in drug metabolism, and overexpression in tumors is associated with significant resistance to many medicinal agents. Consequently, inhibition of P450s could serve as a strategy to restore drug efficacy. However, the widespread expression of P450s throughout the human body and the critical roles they play in various biosynthetic pathways motivates the development of P450 inhibitors capable of controlled local administration. Ruthenium complexes containing P450 inhibitors as ligands were synthesized in order to develop pro-drugs that can be triggered to release the inhibitors in a spatially and temporally controlled fashion. Upon light activation the compounds release ligands that directly bind and inhibit P450 enzymes, while the ruthenium center is able to directly damage DNA.
Zamora, Ana,Denning, Catherine A.,Heidary, David K.,Wachter, Erin,Nease, Leona A.,Ruiz, José,Glazer, Edith C.
p. 2165 - 2173
(2017/02/26)
Enantioselective hydrogenation and transfer hydrogenation of bulky ketones catalysed by a ruthenium complex of a chiral tridentate ligand
A study on the enantioselective hydrogenation of tertiary alkyl ketones catalysed by a novel class of tridentate-Ru complex is reported. In contrast to the extensively studied [RuCl2(diphos)(di-primary amine)] complexes, this new class of hydro
Diaz-Valenzuela, M. Belen,Phillips, Scott D.,France, Marcia B.,Gunn, Mary E.,Clarke, Matthew L.
supporting information; experimental part
p. 1227 - 1232
(2009/08/10)
Heteroditopic imino N-heterocyclic carbenes and their sulfur, selenium, and tungsten tetracarbonyl derivatives
New heterditopic imino N-heterocyclic carbenes for use as chelating ligands in homogeneous catalysis are the focus of this contribution. The synthesis of the corresponding imidazolium precursors is accomplished in three steps by alkylation of imidazole wi
Effect of Anti-Ecdysteroid Azole Analogues of Metyrapone on the Larval Development of the Fleshfly, Neobellieria bullata
Based on our previous finding that PIM (phenyl-imidazolyl-metyrapon; 2-(1-imidazolyl)-2-methyl-1-phenylpropan-1-one, 1) is a strong inhibitor of ecdysone 20-monooxygenase (IC50 = 7.89E-7 M) from the fleshfly, Neobellieria bullata (Parker) and has also a g
Belai, Ivan,Darvas, Bela,Bauer, Krisztina,Tag El-Din, Mahmoud H.
p. 225 - 232
(2007/10/03)
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