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首页> 外文期刊>Medicinal Chemistry >Cellular Pharmacology, Antineoplastic Activity and Low In Vivo Toxicity of a Carboxylato-Bridged Platinum(II) Complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) Dihydrate
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Cellular Pharmacology, Antineoplastic Activity and Low In Vivo Toxicity of a Carboxylato-Bridged Platinum(II) Complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) Dihydrate

机译:羧化桥联铂(II)配合物双(乙酰基)diammine-双-μ-乙酰基二水合铂(II)的细胞药理学,抗肿瘤活性和低体内毒性

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摘要

The dinuclear platinum complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) dihydrate has been previously shown to exert profound cytotoxicity in diverse tumor cell lines, while being far less detrimental than the clinically applied platinum drugs against some susceptible to platinum toxicity non-malignant cellular populations. In the present study we report the investigation of the cellular accumulation kinetics and apoptosis induction of the dinuclear complex in K-562, its potent in vivo antineoplastic activity against L1210 leukemia and Lewis lung carcinoma tumor models and its lower nephrotoxicity, myelosuppresive potential and clastogenicity in vivo relative to cisplatin.
机译:先前已证明,双核铂络合物双(乙酰基)二氨基-双-μ-乙酰基二铂(II)在多种肿瘤细胞系中发挥深远的细胞毒性,但远不如临床上应用的铂类药物对某些易患铂的药物有害。毒性非恶性细胞群。在本研究中,我们报告了对K-562中双核复合物的细胞蓄积动力学和细胞凋亡诱导的研究,其对L1210白血病和Lewis肺癌肿瘤模型的有效体内抗肿瘤活性以及其较低的肾毒性,骨髓抑制潜力和致死性。体内相对于顺铂。

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