Naphthalimide Platinum(IV) Compounds as Antitumor Agents with Dual DNA Damage Mechanism to Overcome Cisplatin Resistance,European Journal of Inorganic Chemistry

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Naphthalimide Platinum(IV) Compounds as Antitumor Agents with Dual DNA Damage Mechanism to Overcome Cisplatin Resistance
European Journal of Inorganic Chemistry ( IF 2.2 ) Pub Date : 2018-10-16 , DOI: 10.1002/ejic.201800799
Qingpeng Wang ₁ , Guoshuai Li ₁ , Zhifang Liu ₁ , Xiaoxiao Tan ₁ , Zhuang Ding ₁ , Jing Ma ₂ , Lanjie Li ₁ , Dacheng Li ₁ , Jun Han ₁ , Bingquan Wang ₁

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A new series of naphthalimide platinum(IV) compounds with dual DNA damage mechanism were designed, synthesized and evaluated for antitumor activities. The platinum(IV) compounds could combine with DNA and cause DNA damage via naphthalimide fragment. Then the platinum(II) complexes released in reductive microenvironment would cause remarkable secondary DNA lesions. Some title compounds exhibit good antitumor activities and are of great potential in overcoming the drug resistance of cisplatin. Furthermore, naphthalimide platinum(IV) complexes could effectively combine with HSA by electrostatic force, which would influence the drug distribution and bioactivities in vivo. Moreover, the accumulation of the tested platinum(IV) compounds in whole cells and DNA is remarkably enhanced in comparison with cisplatin and oxaliplatin.

中文翻译：

萘二甲酰亚胺铂（IV）化合物具有双重DNA损伤机理的抗肿瘤剂，可克服顺铂耐药性

设计，合成并评估了具有双重DNA损伤机理的新系列萘二甲酰亚胺铂（IV）化合物的抗肿瘤活性。铂（IV）化合物可与DNA结合并通过萘二甲酰亚胺片段造成DNA损伤。然后，在还原性微环境中释放的铂（II）配合物将引起显着的继发性DNA损伤。一些标题化合物表现出良好的抗肿瘤活性，并且在克服顺铂的耐药性方面具有巨大潜力。此外，萘二甲酰亚胺铂（IV）配合物可以通过静电力与HSA有效结合，从而影响体内的药物分布和生物活性。此外，与顺铂和奥沙利铂相比，受试铂（IV）化合物在整个细胞和DNA中的积累显着增强。

更新日期：2018-10-16

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