In Vitro Antitumour Activity of Some Triorganophosphinegold(I)Thionucleobases

Abstract

A series of phosphinegold(I) thionucleobase analogues, [R3PAu(SRx)] (R = Et, Ph or chexyl; HSR1 = 2-mercaptobenzoic acid, HSR2 = 2-thiouracil, HSR3 = 6-mercaptopurine and HSR4 = 6-thioguanine) have been examined for their in vitro cytotoxicity in L1210 murine leukemia cells in culture. The range of ID50 values (continuous 48 h exposure) for the complexes is 0.041 - 0.131 μM. The complexes with SR3 and SR4 are generally the most active; however, there is no clear trend associated with the phosphine ligands.

Gold compounds in medicine: Potential anti-tumour agents

“…Preliminary anti-tumour screening, i.e. in vivo was also conducted that showed that activity was maintained to a certain extent (32). The principle of coupling therapeutically important molecules to phosphinegold(I) entities is quite clearly vindicated as may be seen from the data presented in Table 1 (33).…”

“…of triphenylphosphinegold(I) 6-mercaptopurinate, abbreviated as Ph3PAu(6-MP), for these compounds is shown in Figure 6 (14). Several important conclusions were gained from the study of these compounds (31)(32)(33)(34).…”

Organometallic Complexes of Uracil and Orotic Acid Derivatives: Coordination Mode, Structure, and Reactivity

“…[5,6] Metal complexes of pyrimidines have been shown to be useful as biological carriers for some of these drugs such as AZT, [7Ϫ10] others have demonstrated anti-cancer/tumor activity. [11,12] Despite the plethora of coordination complexes of pyrimidines, the organometallic chemistry involving these ligands has received limited attention, with most efforts coming from the laboratory of Beck and co-workers. [13,14] Recently, we have examined the coordination modes of uracils and orotic acid derivatives to zero-valent group-6 carbonylmetal compounds, focusing our studies on the ability of the ring nitrogen atoms to serve as π-donor ligands and to facilitate CO dissociation.…”

Synthesis and cytotoxicity of pyridine and quinoline oxorhenium(V) complexes with tridentate (NS2, S3)/monodentate (s) coordination*

“…As structural fragments they also form part of the structure of the antitumor antibiotics nigrin [1], bruneomycin [2], and antitumor alkaloids camptothecin [3] and meridin [4]. On the other hand, a series of transition metal complexes [5,6], including quinoline-containing [7-10], and also complexes of rhenium [11][12][13], display antitumor activity and are potentially biological transporting agents for medications [14,15].In the present work, with the aim of studying the effect of the ligand nature on antitumor properties, neutral oxorhenium(V) complexes have been synthesized in which the oxorhenium(V) framework ReO 3+ is coordinated with the tridentate 3-thia-and 3-methylazapentane-1,5-dithiolate, and also with the monodentate 2-mercaptopyridine and 2-mercaptoquinoline. The formation of the complexes was carried out by "3+1" methodology using two different rhenium precursors 1 and 2 depending on the neutral donor atom of the tridentate ligand.…”

“…As structural fragments they also form part of the structure of the antitumor antibiotics nigrin [1], bruneomycin [2], and antitumor alkaloids camptothecin [3] and meridin [4]. On the other hand, a series of transition metal complexes [5,6], including quinoline-containing [7][8][9][10], and also complexes of rhenium [11][12][13], display antitumor activity and are potentially biological transporting agents for medications [14,15].…”