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Synthesis and biological evaluation of a series of new germanium phthalocyanines incorporated into liposomes--part I: chemistry

机译:脂质体中掺入的一系列新型锗酞菁的合成和生物学评估-第一部分:化学

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Abstract: Germanium-dihydroxy-phthalocyanine GePc(OH$-2$/) was synthesized and used as starting material for several new, axially disubstituted derivatives of the general formula GePc$LB@OSi(R$- 2$/)R$PRM$RB$-2$/. The preparation of the monosubstituted silanol side chains HOSi(R)$- 2$/R$PRM was performed either by Mitsunobu reaction starting from diphenylsilandiol Si(Ph)$- 2$/(OH)$-2$/ followed by direct coupling of the side-chain with GePc(OH)$-2$/, or by synthesis from a dichlorosilyl derivative. The new compounds were fully characterized and the chemical and main photophysical properties determined. The absorption maxima of these compounds lie in the range of 675 nm. They were found to possess a high quantum efficiency of singlet-oxygen production and fluorescence. The compounds were incorporated into small, unilamellar liposomes following a technology developed by Ciba-Geigy. The dye-to-lipid ratio was 1:100. The liposomal suspensions were freeze-dried for storage. The new compounds were evaluated for their pharmacokinetic and phototherapeutic properties. !15
机译:摘要:合成了锗-二羟基酞菁GePc(OH $ -2 $ /)并将其用作几种通式GePc $ LB @ OSi(R $ -2 $ /)R $ PRM的新型轴向双取代衍生物的原料$ RB $ -2 $ /。单取代的硅烷醇侧链HOSi $ -2 $ / R $ PRM的制备通过Mitsunobu反应进行,从二苯基硅烷二醇Si(Ph)$-2 $ /(OH)$-2 $ /开始,然后直接偶联可以通过GePc(OH)$-2 $ /或通过二氯甲硅烷基衍生物的合成来制备。对新化合物进行了充分表征,并确定了化学和主要光物理性质。这些化合物的最大吸收在675nm的范围内。发现它们具有单线态氧产生和荧光的高量子效率。按照Ciba-Geigy开发的技术,将化合物掺入小的单层脂质体中。染料与脂质的比例为1:100。将脂质体悬浮液冷冻干燥以储存。对新化合物的药代动力学和光疗性质进行了评估。 !15

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