1466-82-6Relevant articles and documents
Synthesis of aspirin-ligated cisplatin derivatives and its slow release study over MIL-101(Fe)
Rosari, Venansia Avelia,Lestari, Witri Wahyu,Firdaus, Maulidan
, p. 2733 - 2741 (2020)
An aspirin-ligated cisplatin derivative, biasplatin, was prepared from acetylsalicylic anhydride and oxoplatin in DMF. Biasplatin was synthesized from oxoplatin and aspirin anhydride as starting materials by a substitution reaction of hydroxo leaving groups in its axial position. The obtained biasplatin was fully characterized by FTIR, 1HNMR, 13CNMR, and ESI mass spectroscopy. Biasplatin entrapped into MIL-101(Fe) by suspended in DMF and stirring for 72?h at ambient temperature, known as biasplatin@MIL-101(Fe). The slow release of biasplatin and biasplatin@MIL-101(Fe) was conducted in PBS solution pH 7.20, 37?°C as media and measured by UV–Vis spectrophotometer. The release of biasplatin without loaded into MIL-101(Fe) is persistent for 3%, and biasplatin@MIL-101(Fe) is 0.05% over 72?h. A significant slow release of biasplatin@MIL-101(Fe) only 1% compared with time release of biasplatin without loaded into MIL-101(Fe).
Ctc-[Pt(NH3)2(cinnamate)(valproate)Cl2] is a highly potent and low-toxic triple action anticancer prodrug
Li, Yang,Shi, Shan,Zhang, Shurong,Gan, Zongjie,Wang, Xin,Zhao, Xudong,Zhu, Yijian,Cao, Meiting,Wang, Xiaoyue,Li, Wei
supporting information, p. 11180 - 11188 (2021/08/25)
Pt(iv) prodrugs have gained tremendous attention due to their indisputable advantages compared to cisplatin. Herein, new Pt(iv) derivatives with cinnamic acid at the first axial position, and inhibitor of matrix metalloproteinases-2 and-9, histone deacetylase, cyclooxygenase or pyruvate dehydrogenase at the second axial position are constructed to develop multi-action prodrugs. We demonstrate that Pt(iv) prodrugs are reducible and have superior antiproliferative activity with IC50 values at submicromolar concentrations. Notably, Pt(iv) prodrugs exhibit highly potent anti-tumour activity in an in vivo breast cancer model. Our results support the view that a triple-action Pt(iv) prodrug acts via a synergistic mechanism, which involves the effects of CDDP and the effects of axial moieties, thus jointly leading to the death of tumour cells. These findings provide a practical strategy for the rational design of more effective Pt(iv) prodrugs to efficiently kill tumour cells by enhancing their cellular accumulation and tuning their canonical mechanism.
PRODRUG FOR RELEASE OF CISPLATIN AND CYCLOOXYGENASE INHIBITOR
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Paragraph 0098, (2015/06/25)
Pt(IV) prodrugs include one or more conjugated cyclooxygenase inhibitor. Reduction of Pt(IV) to Pt(II) can result cisplatin and a cyclooxygenase inhibitor. For proof of concept, a Pt(IV) prodrug that can produce cisplatin and aspirin, Platin-A, was synthesized. Platin-A exhibited excellent anticancer and anti-inflammatory properties, which were better than the combination of free formulation of cisplatin and aspirin.
