66845-32-7

Usage

Uses

Used in Oncology:
Nsc290127 is used as an antitumor agent for its activity against colorectal cancer. Its cytotoxicity is attributed to the formation of adducts with DNA, which helps inhibit tumor growth and progression.
Used in Drug Development:
As an impurity of Oxiplatin, Nsc290127 plays a role in the development and understanding of the therapeutic effects and potential side effects of platinum-based chemotherapy drugs. Further research on its properties and interactions with biological systems can contribute to the optimization of cancer treatment strategies.

InChI:InChI=1/C6H12N2.2HI.Pt/c7-5-3-1-2-4-6(5)8;;;/h5-8H,1-4H2;2*1H;/q-2;;;+4/p-2/rC6H12N2.I2Pt/c7-5-3-1-2-4-6(5)8;1-3-2/h5-8H,1-4H2;/q-2;+2

Upstream product

• 694-83-7 rac-diaminocyclohexane 
• 7681-11-0 potassium iodide 
• 10025-99-7 potassium tetrachloroplatinate(II) 
• 1121-22-8 trans-1,2-Diaminocyclohexane 

Downstream Products

• 66900-71-8 (dach)Pt(SO₄) 
• 38780-40-4 {(1R,2R)-cyclohexane-1,2-diamine}dichloridoplatinum(II) 
• 61848-66-6 cis-dichloro-(cis-1,2-diaminocyclohexane)platinum(II) 
• 1428416-33-4 [2-(2-diethylaminoethyl)succinato][cis-(1,2-trans-cyclohexanediamine)]platinum(II) tosylate 

Relevant academic research and scientific papers

In vitro and in vivoactivity of series of cationic dinuclearPt(II) complexes

The antitumour potential of nine dinuclear platinum(II) complexes of the type [{Pt(L)Cl}2(μ-X)]2+(where L represents two NH3 or different bidentantly coordinated diamine ligand - ethylenediamine, en; (±)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(±)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2-dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd; (±)-1,3-pentanediamine,1,3-pnd, and X is a bridging pyrazine (pz) or pyridazine (pydz) ligand) were determined by in vitro and in vivo assays using the CT26 cell line and a murine model of heterotopic colon cancer tumour induced in immunocompetent BALB/c mice. This study concludes that complexes Pt1, Pt2 and Pt7 possess significant in vitro cytotoxic activity against mouse colon carcinoma CT26 cells, while all these complexes show moderate apoptotic effect. Complexes Pt1 and Pt7 arrested CT26 cells in G2/M phase of cell cycle, while, evaluated by detection of Ki67 expressing cells, complexes Pt5 and Pt6 exerted the highest antiproliferative effect. Complexes Pt1 and Pt2 exerted significant in vivo antitumour effects. These complexes reduced the growth of primary tumour and the incidence of lung and liver metastases without causing the significant hepato- and nephro- toxicity. Our data indicate considerable antitumour activity of platinum(II) complexes against CT26 cells in vitro and in vivo and imply possible further investigations on their role as potential chemotherapeutic agents.

Synthesis, cytotoxic activity and DNA interaction studies of new dinuclear platinum(ii) complexes with an aromatic 1,5-naphthyridine bridging ligand: DNA binding mode of polynuclear platinum(ii) complexes in relation to the complex structure

The synthesis, spectroscopic characterization, cytotoxic activity and DNA binding evaluation of seven new dinuclear platinum(ii) complexes Pt1-Pt7, with the general formula [{Pt(L)Cl}2(μ-1,5-nphe)](ClO4)2 (1,5-nphe is 1,5-naphthyridine; while L is two ammines (Pt1) or one bidentate coordinated diamine: ethylenediamine (Pt2), (±)-1,2-propylenediamine (Pt3), trans-(±)-1,2-diaminocyclohexane (Pt4), 1,3-propylenediamine (Pt5), 2,2-dimethyl-1,3-propylenediamine (Pt6), and 1,3-pentanediamine (Pt7)), were reported. In vitro cytotoxic activity of these complexes was evaluated against three tumor cell lines, murine colon carcinoma (CT26), murine mammary carcinoma (4T1) and murine lung cancer (LLC1) and two normal cell lines, murine mesenchymal stem cells (MSC) and human fibroblast (MRC-5) cells. The results of the MTT assay indicate that all investigated complexes have almost no cytotoxic effects on 4T1 and very low cytotoxicity toward LLC1 cell lines. In contrast to the effects on LLC1 and 4T1 cells, complexes Pt1 and Pt2 had significant cytotoxic activity toward CT26 cells. Complex Pt1 had a much lower IC50 value for activity on CT26 cells compared with cisplatin. In comparison with cisplatin, all dinuclear Pt1-Pt7 complexes showed lower cytotoxicity toward normal MSC and MRC-5 cells. In order to measure the amount of platinum(ii) complexes taken up by the cells, we quantified the cellular platinum content using inductively coupled plasma mass spectrometry (ICP-QMS). Molecular docking studies performed to evaluate the potential binding mode of dinuclear platinum(ii) complexes Pt1-Pt7 and their aqua derivatives W1-W7, respectively, at the double stranded DNA showed that groove spanning and backbone tracking are the most stable binding modes.

A method for the treatment of tumor cell proliferative diseases of platinum (II) compound

Disclosed are a platinum compound with the leaving group malonic derivative "2" position substituent containing a primary amino, a secondary amino, a tertiary amino, and a quaternary amino, as well as pharmaceutically acceptable salt, preparation method thereof, and pharmaceutical composition containing the compound. Also disclosed are uses of the compound for treating cell proliferative diseases, particularly cancers. The platinum compound of the present invention has the high water solubility and the low toxicity.

Synthesis and evaluation of series of diazine-bridged dinuclear platinum(II) complexes through in vitro toxicity and molecular modeling: Correlation between structure and activity of pt(II) complexes

Polynuclear Pt(II) complexes are a novel class of promising anticancer agents with potential clinical significance. A series of pyrazine (pz) bridged dinuclear Pt(II) complexes with general formulas {[Pt(L)Cl]2(μ-pz)}2+ (L, ethylenediamine, en; (±)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(±)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2-dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd) and one pyridazine (pydz) bridged {[Pt(en)Cl]2(μ-pydz)}2+ complex were prepared. The anticancer potential of these complexes were determined through in vitro cytotoxicity assay in human fibroblasts (MRC5) and two carcinoma cell lines (A375 and HCT116), interaction with double stranded DNA through in vitro assay, and molecular docking study. All complexes inhibited cell proliferation with inhibitory concentrations in the 0.5-120 μM range. While {[Pt(1,3-pd)Cl]2(μ-pz)}2+ showed improved activity and {[Pt(en)Cl]2(μ-pydz)}2+ showed comparable activity to that of clinically relevant cisplatin, {[Pt(en)Cl]2(μ-pydz)}2+ was less toxic in an assay with zebrafish (Danio rerio) embryos, causing no adverse developmental effects. The in vitro cytotoxicity of all diazine-bridged dinuclear Pt(II) complexes is discussed in correlation to their structural characteristics.

PLATINUM COMPOUND OF MALONIC ACID DERIVATIVE HAVING LEAVING GROUP CONTAINING AMINO OR ALKYLAMINO

Disclosed are a class of platinum compounds of malonic acid derivatives having a leaving group containing an amino or alkylamino, and pharmaceutically acceptable salt thereof, preparation method thereof and pharmaceutical composition containing the compou

PLATINUM COMPOUND HAVING AMINO- OR ALKYLAMINO-CONTAINING SUCCINIC ACID DERIVATIVES AS LEAVING GROUP, PREPARATION METHOD THEREFOR, AND USE THEREOF

Disclosed are a category of platinum compounds having amino- or alkylamino-containing succinato derivatives as leaving group, or pharmaceutically acceptable salts thereof, preparation method thereof, and medicinal compositions containing the compounds. Also disclosed is a use of the compounds in treating cell proliferative diseases, especially cancers. The platinum compounds of the present invention have high water solubility and small toxic side effect.

PLATINUM COMPOUNDS FOR TREATING CELL PROLIFERATIVE DISEASE, PREPARATION METHODS AND USES THEREOF

Disclosed are a class of platinum compounds with a leaving group of malonic acid derivatives containing amino and alkylamino, their pharmaceutically acceptable salts, their preparation methods and pharmaceutical composites comprising them. Disclosed also are for the uses of the compounds in the treatment of cell proliferative diseases, particularly for the treatment of cancers. The present platinum compounds have high water solubility and low toxicity.

Molecular interaction fields vs. quantum-mechanical-based descriptors in the modelling of lipophilicity of platinum(iv) complexes

We report QSAR calculations using VolSurf descriptors to model the lipophilicity of 53 Pt(iv) complexes with a diverse range of axial and equatorial ligands. Lipophilicity is measured using an efficient HPLC method. Previous models based on a subset of these data are shown to be inadequate, due to incompatibility of whole molecule descriptors between carboxylato and hydroxido ligands. Instead, the interaction surfaces of complexes with various probes are used as independent descriptors. Partial least squares modelling using three latent variables results in an accurate (R2 = 0.92) and robust model (Q2 = 0.87) of lipophilicity, that moreover highlights the importance of size and hydrophobicity terms and the modest relevance of hydrogen bonding.

Metal-polysaccharide conjugates: compositions, synthesis and methods for cancer therapy

The current disclosure, in one embodiment, includes a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid. According to another embodiment, the disclosure provides a method of synthesizing a polysaccharide conjugate by covalently bonding a monomeric amino acid having an O-group to a polysaccharide and by conjugating a metal to the O-group to form a polysaccharide conjugate. According to a third embodiment, the disclosure relates to a method of killing a cancer cell by administering to the cell an effective amount of a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid.

BENZOISOSELENAZOLE DERIVATIVES WITH ANTI-INFLAMMATION, ANTIVIRUS AND ANTI-THROMBOSIS ACTIVITY AND THEIR USE

The present invention relates to new bisbenzisoselenazolonyl derivatives of the following general formulae (I), (II) or (III) and their pharmaceutically acceptable salts. The inventive derivatives have antineoplastic, anti-inflammatory and antithrombotic activities.