111263-58-2Relevant academic research and scientific papers
Platinum(iv) prodrugs with long lipid chains for drug delivery and overcoming cisplatin resistance
Chen, Qiling,Yang, Yuanyuan,Lin, Xun,Ma, Wen,Chen, Gui,Li, Wenliang,Wang, Xuefeng,Yu, Zhiqiang
, p. 5369 - 5372 (2018)
Platinum(iv) prodrugs of clinically used cisplatin and oxaliplatin with two axial long lipid chains were developed for nanoparticle delivery to combat cisplatin resistance.
Preparation method and application of compounds and anticancer drugs
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Paragraph 0058-0059, (2021/10/27)
The invention provides compounds, which are twin drugs formed by a platinum drug and a small molecule drug covalently connected to the axial position of the platinum drug and having an immune negative modulation relieving function, and have structures as shown in a formula I: wherein the structure of the platinum drug is in a dotted frame; R1 and R2 are the same or different small molecule drugs with the function of relieving immune negative regulation; or one of R1 and R2 is a small molecule medicine with an immune negative regulation relieving function, and the other one is hydroxyl. According to the invention, the small molecule drug with the function of relieving the negative immune regulation is covalently linked to the axial position of the platinum drug to form the twin drug, so that the tumor killing effect of the platinum drug and the function of relieving the negative immune regulation of the small molecule drug are simultaneously exerted at the tumor site; the twin drugs are combined with immunotherapy for use, so that the response of immunotherapy can be effectively improved, and the treatment effect on tumors is remarkably improved. The platinum anticancer twin drug are simple in preparation method, low in cost and suitable for industrial production, and has clinical transformation potential.
Pegylated ICD inducer-IDO inhibitor nano conjugate as well as preparation method and application thereof
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Paragraph 0066; 0071; 0072; 0076, (2020/05/01)
The invention discloses a pegylated ICD inducer-IDO inhibitor nano conjugate as well as a preparation method and application thereof. The structural formula of the pegylated ICD inducer-IDO inhibitornano conjugate is shown in the specification, wherein R is H or a substance shown in the specification, and the weight-average molecular weight is 1000-5000. According to the pegylated ICD inducer-IDOinhibitor nano conjugate provided by the invention, in a water-based medium, a pegylated drug conjugate can be self-assembled into a drug-based nano conjugate. Not only can non-specific accumulationin MPS-related organs be reduced, but also the passive targeting ability to solid tumors is improved through enhanced permeability and retention effect, so that the treatment index is improved.
Glucose-conjugated platinum(IV) complexes as tumor-targeting agents: design, synthesis and biological evaluation
Wang, Haifeng,Yang, Xiande,Zhao, Caili,Wang, Peng George,Wang, Xin
, p. 1639 - 1645 (2019/03/08)
A new series of glucose-conjugated Pt(IV) complexes that target tumor-specific glucose transporters (GLUTs) was designed, synthesized, and evaluated for their anticancer activities. All six compounds, namely, A1-A6, exhibited increased cytotoxicity that w
Compound having asymmetric mono-substituted coumarin tetravalent platinum structure, preparation method thereof and use thereof in preparation of antitumor drugs
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Paragraph 0046-0048, (2019/11/19)
A compound having an asymmetric mono-substituted coumarin tetravalent platinum structure has a structural formula as shown in the description. A preparation method of the compound having an asymmetricmono-substituted coumarin tetravalent platinum structure specifically comprises the following steps: adding TBTU and a coumarin derivative to a reaction container, replacing air in the system with nitrogen, adding dried DMF for stirred reaction for about 10 minutes at room temperature, adding dried triethylamine to the reaction system for stirred reaction for about 10 minutes at room temperature,finally adding a tetravalent platinum compound to the reaction system, replacing air in the flask with N2 and putting the reaction system at 25-120 DEG C for light-shielded reaction for 12-72 hours,removing the solvent under reduced pressure, and carrying out column chromatography to obtain an asymmetric mono-substituted coumarin modified tetravalent platinum compound having the general formula(1).
5 - Fluorouracil - platinum (IV) complex, intermediate, preparation method and application thereof (by machine translation)
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Paragraph 0177; 0179; 0180; 0181, (2019/04/09)
The present invention provides 5 - fluoro uracil - platinum (IV) complex, intermediate and preparation method, by formula (1) expressed, wherein Is selected from cisplatin, oxaliplatin, carboplatin, age platinum, nedaplatin or Miboplatin, preferred, For cisplatin or oxaliplatin; R1 For - Cn H2 N -, N is an integer and n ≥ 1, preferred, - Cn H2 N - Straight chain group, R2 For - Cm H2 M + 1 , M is an integer and m ≥ 1, preferred, - Cm H2 M + 1 Straight chain group. The invention of 5 - Fluorouracil - platinum (IV) complex can be reduced cisplatin, oxaliplatin with 5 - Fluorouracil toxic side effect, and at the same time used for the treatment of cancer and in anti-tumor drugs have the synergistic the sensitivity. (by machine translation)
Carbonic anhydrase-targeted Pt (IV) complex, preparation method and application thereof
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Paragraph 0074; 0076, (2019/10/01)
The invention discloses a carbonic anhydrase (CAIX) targeted Pt (IV) complex as well as a preparation method and application thereof. The invention firstly provides the CAIX-targeted Pt (IV) complex which has the targeting characteristic of CAIX, can specifically identify tumor cells, effectively inhibit the activity of CAIX, is non-toxic to normal cells, enhances the toxicity under the conditionof anoxia, and has remarkable antitumor activity. Compared with a Pt (II) drug, the complex has the characteristics of improving tumor selectivity, reducing liver injury, reducing renal toxicity and having no toxic or side effect, and can be specifically combined with an anti-tumor target, so that the sensitivity of the platinum drug in a hypoxia environment is improved. The invention also provides a preparation method of the complex, which comprises the following steps of: mixing CAIXi and Pt (IV) - COOHx in a DMF solution containing N,N-diisopropylethylamine, and carrying out condensation reaction to obtain the complex. The preparation method is simple and low in cost. The product has a good antitumor drug application prospect and a wide development space.
Mono-functionalized glycosylated platinum(IV) complexes possessed both pH and redox dual-responsive properties: Exhibited enhanced safety and preferentially accumulated in cancer cells in?vitro and in?vivo
Ma, Jing,Yang, Xiande,Hao, Wenpei,Huang, Zhonglv,Wang, Xin,Wang, Peng George
, p. 45 - 55 (2017/02/05)
A serious of carbohydrate-conjugated platinum(IV) complexes in the form Pt(L2)(A2)(OH)R based on the clinical drug cisplatin and oxaliplatin were designed, synthesized and evaluated as antitumor agents in?vitro and in?vivo. The conjugates possessing both pH and redox dual-responsive properties exhibited more potent cytotoxicity in seven different human cancer cell lines and lower toxicity to the normal 3T3 cells than cisplatin, oxaliplatin and even the reported bis-functionalized glycosylated platinum(IV) complexes indicating the enhanced safety of the sugar conjugates. Cellular drug uptake and DNA platination were also superior to cisplatin, oxaliplatin and the reported bis-functionalized ones. Peak current of B7 and B8 with the scan rate of 200mv/s at the concentration of 0.08?mM was 5-fold higher at pH 6.4 than the pH 7.4, indicating that carbohydrate-conjugated mono-functionalized platinum(IV) complexes possessed both pH and redox dual-responsive properties in the cancer cells. The in?vivo assays demonstrated that the Pt(IV) compounds could inhibit the growth of MCF-7 tumour and exert more safety than oxaliplatin.
Platinum (IV) anticancer compounds with dihydrogen phosphate radical as axial ligand
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Paragraph 0050; 0051, (2016/12/01)
The invention relates to platinum (IV) anticancer compounds with a dihydrogen phosphate radical as an axial ligand. The chemical structure of the compounds is shown in the description. In the structure, a carrier group 2A is an ammonia/amine liand, and comprises 2NH3, 1R,2R-cyclohexanediamin, 1,2-bis(aminomethyl)cyclobutane, NH3/cyclopentamine and NH3/cyclohexylamine; and leaving groups 2X are the leaving groups of platinum (II) anticancer compounds existing at present, and comprise 2Cl, an oxalate radical, a 1,1-cyclobutanedicarboxylate radical and a propane dicarboxylate radical. Phosphoric acid bonding is helpful for running of compounds to cancer cell nuclei, improving the selectivity of cancer cells, and makes the compounds mediate compound targeting osteocarcinoma and have very strong anticancer effect. The compounds have the advantages of good water solubility and stability, and are highly suitable for being used as anticancer drugs.
Platinum(IV) complexes featuring one or two axial ferrocene bearing ligands - Synthesis, characterization, and cytotoxicity
Banfic?, Jelena,Legin, Anton A.,Jakupec, Michael A.,Galanski, Markus,Keppler, Bernhard K.
, p. 484 - 492 (2014/02/14)
Ferrocenyl compounds show interesting antiproliferative properties. Consequently, ferrocene bearing moieties were prepared and coupled for the first time to anticancer platinum(IV) complexes. The compounds, featuring either one or two axially coordinated ferrocene-containing ligands, were fully characterized by ESI-MS and multinuclear (1H, 13C, 15N, and 195Pt) one- and two-dimensional NMR spectroscopy. Their cytotoxicity was investigated in three human cancer cell lines deriving from ovarian carcinoma (CH1), colon carcinoma (SW480), and non-small-cell lung carcinoma (A549) by means of the colorimetric MTT assay. Promising IC 50 values in the low micromolar range in CH1 and SW480 human cancer cells were found. Copyright
