Modified 5′-Trityl Nucleosides as Inhibitors of<i>Plasmodium falciparum</i>dUTPase
作者:Gian Filippo Ruda、Corinne Nguyen、Przemysław Ziemkowski、Krzysztof Felczak、Ganasan Kasinathan、Alexander Musso-Buendia、Christian Sund、Xiao Xiong Zhou、Marcel Kaiser、Luis M. Ruiz-Pérez、Reto Brun、Tadeusz Kulikowski、Nils Gunnar Johansson、Dolores González-Pacanowska、Ian H. Gilbert
DOI:10.1002/cmdc.201000445
日期:2011.2.7
2′‐Deoxyuridine triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for the treatment of malaria. We previously reported the discovery of 5′‐tritylated analogues of deoxyuridine as selective inhibitors of this Plasmodiumfalciparum enzyme. Herein we report further structure–activity studies; in particular, variations of the 5′‐trityl group, the introduction of various substituents
Syntheses and ultraviolet spectra of N-organosilyl ketimines
作者:Liu-Heung Chan、Eugene G. Roschow
DOI:10.1016/s0022-328x(00)83725-0
日期:1967.8
Twenty eight silyl ketimines and several germanium and tin analogs have been prepared by the action of sodium bis(trimethylsilyl)amide on non-enolizable ketones or the reaction of lithium derivatives of ketimines with organosilicon chlorides. Their electronic spectra, the n→π* transition in particular, have been investigated to the d*-p* interaction between the empty d orbitals of silicon and the π
通过双(三甲基甲硅烷基)酰胺钠对不可烯化的酮的作用或酮亚胺的锂衍生物与有机硅氯化物的反应,已经制备了二十八个甲硅烷基酮亚胺以及几种锗和锡的类似物。其电子光谱中,Ñ →π *在特定的转换,已研究了对d * - p *空间相互作用d硅的轨道和CN键的π体系。光谱数据表明CN·Si键的弯曲结构,因此Si·N键中很少有多重键。
Synthesis, Hydrolytic Reactivity, and Anticancer Evaluation of N- and O-Triorganosilylated Compounds as New Types of Potential Prodrugs
作者:Fang-Ting Chiu、Young Hwan Chang、Günay Ӧzkan、Gerald Zon、Kenneth C. Fichter、Lawrence R. Phillips
DOI:10.1002/jps.2600710517
日期:1982.5
N- and O-Triorganosilylatedcompounds related to various anticancer agents were synthesized for evaluation as potentialanticancerprodrugs. 1H-NMR and UV kinetic measurements of hydrolytic desilylation were used to correlate relative rates of structural unmasking with steric bulk about the silicon reaction center. The tert-butyldimethylsilyl ester of chlorambucil and a number of O- triorganosilylated
A process is described for converting the C(7) hydroxy group of a 10-acyloxy-7-hydroxytaxane to an acetal or ketal, the process comprising treating the 10-acyloxy-7-hydroxytaxane with a ketalizing agent in the presence of an acid catalyst to form a C(7) ketalized taxane of the formula
or
wherein either X31 or X32 represents the 10-acyloxy-7-hydroxytaxane moiety and the other of X31 and X32 as well as X33 and X34 are independently hydrocarbyl, substituted hydrocarbyl or heteroaryl moieties. Taxanes having a ketalized C(7) hydroxy group are also described.