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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate.
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Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate.

机译：3,5-二异丙基水杨酸酯的亲脂性铂（II）配合物的合成及其抗癌活性。

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摘要

Novel lipophilic platinum(II) complexes (LSPt-1-3), containing 3,5-diisopropylsalicylate (DIPS) as a leaving group and 2NH(3) or 1R,2R-diaminocyclohexane or (4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane as the carrier, have been synthesized, characterized and evaluated in vitro and in vivo. The octanol/water distribution coefficient of the complexes has also been measured. The results showed that the complexes achieved a typical square planar and the octanol/water distribution coefficient logP was 4.27, 4.37 and 4.31. The complexes were tested by SRB method to be more cytotoxic than Carboplatin, Oxaliplatin and Eptaplatin against 3AO, A549, NCI-H460 and SGC-7901 human cancer cell lines. Among complexes, LSPt-2 was much more effective than Carboplatin and Oxaliplatin in treating the NCI-H460 non-small-cell lung tumor-bearing mice. Its optimal activity was 38.8% (T/C) at a dose of 30 mg/kg following i.p. administration. LD(50) for the complex was found to be 230.9 mg/kg. LSPt-2 exhibited great anticancer activity, good lipophilic ability and low toxicity and therefore, it is a promising candidate for effective and stable pharmaceutical liposomal platinum anticancer drug.
机译：新型亲脂性铂（II）配合物（LSPt-1-3），包含3,5-二异丙基水杨酸酯（DIPS）作为离去基团和2NH（3）或1R，2R-二氨基环己烷或（4R，5R）-4,5-已在体外和体内合成，表征和评估了以双（氨基甲基）-2-异丙基-1,3-二氧戊环为载体。还测量了配合物的辛醇/水分配系数。结果表明，该配合物达到了典型的正方形平面，辛醇/水的分配系数logP为4.27、4.37和4.31。通过SRB方法测试该复合物对3AO，A549，NCI-H460和SGC-7901人癌细胞的细胞毒性比卡铂，奥沙利铂和埃铂更高。在复合物中，LSPt-2在治疗NCI-H460非小细胞肺癌小鼠中比卡铂和奥沙利铂更有效。腹腔注射后30 mg / kg的最佳活性为38.8％（T / C）。行政。该复合物的LD（50）为230.9 mg / kg。 LSPt-2具有很好的抗癌活性，亲脂性好，毒性低，因此是有效，稳定的脂质体铂类抗癌药物。

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