- Combating metastasis of breast cancer cells with a carboplatin analogue containing an all-trans retinoic acid ligand
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Pt-ATRA, a carboplatin analogue containing an all-trans retinoic acid (ATRA) derivative ligand, was synthesized via a click reaction. Upon cellular internalization, Pt-ATRA exhibits a dual function, releasing an active Pt(ii) moiety to induce cell apoptosis and ATRA to inhibit tumor metastasis.
- Cheng, Junjie,Dai, Yi,Huang, Hai,Liu, Yangzhong,Shen, Ai-Zong,Zhu, Yang
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Read Online
- A novel platinum-based liposome preparation, and its preparation method
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The invention relates to a novel platinum compound, a liposome preparation containing the compound, a preparation method of the liposome preparation and an application of the liposome preparation in tumor treatment. The main components of the platinum liposome provided by the invention include active platinum compounds, phospholipid, cholesterol, fatty acid and the like, the platinum liposome can be prepared into a freeze-dried powder injection by freeze drying, and the platinum liposome is small in particle size, high in medicine loading capacity and good in stability. The platinum liposome can improve the bioavailability of cisplatin liposome, prolong the residence time of the medicine in vivo and concentrate the cisplatin in cancerous organs, thereby not only reducing the medicine dosage and reinforcing the curative effect, but also capable of reducing the toxic side effects of the medicine, so that the platinum liposome is suitable for treating a variety of tumor diseases.
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Paragraph 0061; 0062
(2017/02/24)
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- Synthesis, characterization, structures and cytotoxicity of platinum(II) complexes containing dimethylpyrazole based selenium ligands
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A series of water soluble platinum(II) complexes of general formulae [Pt(en)(L)][NO3]2, [Pt(NH3)2(L)][NO3]2 [en = ethylenediamine; L = dmpzC6H4Se(CH2)nCOOH or dmpzCH2CH2Se(CH2)nCOOH (n = 1 and 2)], [Pt(en)(L)][NO3][OH]·H2O [L = dmpzCH2CH2Se(CH2)nCOOH (n = 1 and 2)] and [Pt(dmpzCH2CH2SeCH2CH2COOH)2][Cl]2·2H2O have been synthesized. They were characterized by microanalyses, IR, NMR (1H, 13C{1H}, 77Se{1H} and 195Pt{1H}) spectroscopy. Molecular structures of [Pt(en)(dmpzCH2CH2SeCH2COOH)][NO3][OH]·H2O and [Pt(dmpzCH2CH2SeCH2CH2COOH)2][Cl]2·2H2O were determined unambiguously by single crystal X-ray diffraction analyses. The cytotoxicity of these complexes has been evaluated against human colon (HT29, Colo205), ovarian (A2780) and bladder (T24) cancer cell lines and compared with the activity of cisplatin and adriamycin.
- Chopade, Suresh M.,Phadnis, Prasad P.,Hodage, Ananda S.,Wadawale, Amey,Jain, Vimal K.
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supporting information
p. 72 - 80
(2015/02/19)
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- CARRIER THAT TARGETS FUCOSYLATED MOLECULE-PRODUCING CELLS
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The present invention relates to a carrier that is targeted at fucosylated molecule-producing cells, which comprises an effective amount of fucose for targeting said cells, to a composition comprising the carrier, and to a method for treating and diagnosing a disease related to fucosylated molecule-producing cells utilizing said carrier, etc. The carrier of the present invention enables to deliver a substance specifically to fucosylated molecule-producing cells.
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Paragraph 0139
(2015/02/18)
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- PARTUCULATE CONSTRUCTS FOR RELEASE OF ACTIVE AGENTS
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Particulate constructs stabilized by amphiphilic copolymers and comprising at least one active coupled to a hydrophobic moiety provide sustained release of the active in both in vitro and in vivo environments.
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Page/Page column 39
(2008/06/13)
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- Platinum carboxylate anticancer compounds
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Platinum carboxylate anticancer compounds, pharmaceutical compositions that include the platinum carboxylate compounds, and methods for treating cellular proliferative diseases by administering the platinum carboxylate compounds.
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Page/Page column 8-9
(2008/06/13)
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- Synthesis, characterization, and biological activity of cis-diammineplatinum(II) complexes of the DNA intercalators 9-aminoacridine and chloroquine
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The anticancer drug cis-diamminedichloroplatinum(II) reacts with the DNA intercalators 9-aminoacridine (9-AA) and chloroquine (CQ) to form the novel complexes cis-[Pt(NH3)2(N9-9-AA)Cl](NO3) (1), cis-[Pt(NH3)2(N9-9-AA)2](NO3) 2 (2), and cis-[Pt(NH3)2(N1-HCQ)Cl](NO3)2 (3). Interestingly, platinum coordinates to the deprotonated exocyclic amino group of 9-aminoacridine in 1 and 2, with the proton being transferred to the endocyclic nitrogen atom N10, as revealed by X-ray crystal structure determinations. As a consequence, the acridine rings are asymmetrically positioned with respect to the platinum coordination plane, resulting in short (2.390 ? in 1-MeOH and 2.458 A1? in 2-MeOH) nonbonded contacts between platinum and one of the acridine ring protons (H1). NMR spectroscopic studies demonstrated the persistence of this structure in DMF solutions of the complexes, the short Pt-H1 distances resulting in paramagnetic deshielding of the H1 protons by approximately 3.32 (1) and 2.25 (2) ppm. The Pt-H1 interactions are not agostic, however, since no reduction in the magnitude of 1JC1-H1 coupling is observed. In contrast to 9-aminoacridine, chloroquine preferentially coordinates to platinum via the less hindered endocyclic N1 ring nitrogen atom. Since both diastereoisomers of 3 are observed by 1H NMR spectroscopy, rotation about the Pt-N1 bond is slow on the NMR time scale. Complexes of the general formula Cis-[Pt(NH3)2(INT)Cl]n+, where INT is a DNA intercalator such as 9-AA or CQ, have the potential to bind both covalently and intercalatively to DNA and, consequently, are potential antitumor agents. Complexes 1 and 3 were determined to be extremely toxic in animal screens, however, precluding their use as drugs.
- Sundquist, Wesley I.,Bancroft, Daniel P.,Lippard, Stephen J.
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p. 1590 - 1596
(2007/10/02)
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