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Sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells and preparation method and application thereof

A drug-resistant cell and anti-tumor technology, which is applied in the fields of anti-tumor drugs, pharmaceutical formulations, platinum group organic compounds, etc., can solve the problems of undiscovered anti-tumor activity research, and achieve superior anti-tumor activity in vitro

Active Publication Date: 2018-11-09
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Judging from the current research, there is no relevant report on the complexes and anti-tumor activity studies using it as the active ligand.

Method used

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  • Sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells and preparation method and application thereof
  • Sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells and preparation method and application thereof
  • Sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 1.0mmol ligand SFB and 1.0mmol cis-PtCl respectively 2 (DMSO) 2 , placed in a 100.0mL high-temperature pressure-resistant bottle, add 25.0mL of anhydrous methanol and 5.0mL of acetone solution, heat at 45°C for 28 hours, cool to room temperature, a large amount of yellow product precipitates, suction filter, yellow The product was washed successively with methanol, acetone and ether, and dried under vacuum at 45°C to finally obtain complex 1 with a yield of 98.0%.

[0027] Identification of the obtained complex 1:

[0028] (1) Infrared spectrum, its spectrogram is as follows figure 1 shown.

[0029] IR(KBr):3348,3080,2920,2563,1711,1615,1547,1484,1418,1303,1254,1198,1176,1134,1050,1030,944,848,663,535,436cm -1 .

[0030] (2) Electrospray mass spectrometry, its spectrogram is as figure 2 shown.

[0031] ESI-MS m / z:884.6[M-H+DMSO] - , where M is the molecular weight of complex 1.

[0032] (3) Proton NMR spectrum, such as image 3 shown.

[0033] 1 H NMR...

Embodiment 2

[0042] Weigh the ligands 1.0mmol SFB and 5.0mmol cis-PtCl respectively 2 (DMSO) 2 , placed in a 100.0mL high-temperature and pressure-resistant bottle, add 50.0mL of absolute ethanol and 10.0mL of acetone solution, heat at 65°C for 36 hours, cool down to room temperature, a large amount of yellow product precipitates, and suction filter, The yellow product was washed successively with methanol, acetone and ether, and dried under vacuum at 45°C to finally obtain complex 1 with a yield of 85.5%.

Embodiment 3

[0044] Weigh 5.0mmol ligand SFB and 1.0mmol cis-PtCl respectively 2 (DMSO) 2 , placed in a 100.0mL high-temperature and pressure-resistant bottle, add 40.0mL of acetonitrile and 20.0mL of acetone solution, heat at 37°C for 12 hours, cool down to room temperature, a large amount of yellow product precipitates, suction filter, yellow product After washing with methanol, acetone and ether in sequence, and vacuum drying at 45°C, complex 1 was finally obtained with a yield of 75.0%.

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PUM

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Abstract

A sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells is disclosed. The chemical structure of the complex is shown as follows in the description. The complex shows excellent antitumor activity in vitro, has potential medicine value and can be used for preparing various antitumor medicines.

Description

technical field [0001] The invention relates to the field of drugs targeting drug-resistant human lung cancer cells and its preparation method, in particular Sorafenib anti-tumor platinum (II) complexes targeting drug-resistant human lung cancer cells and its preparation method and application. Background technique [0002] In 1965, American biophysicist Rosenberg and others accidentally discovered that "inert platinum electrodes" can promote bacterial growth, and thus started research on the anticancer activity and mechanism of cisplatin. Cisplatin can bind to nuclear DNA, inhibit DNA replication, and damage the cell membrane structure. It has strong broad-spectrum anticancer properties and has good curative effects on ovarian cancer, nasopharyngeal cancer, testicular cancer, head and neck cancer, and lung cancer. Synthesize thousands of platinum complexes, among which carboplatin, nedaplatin and oxaliplatin are widely used clinically. Although these platinum complexes have...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCA61P35/00C07F15/0093
Inventor 覃其品谭明雄王书龙王振凤罗冬妹吕艳廖凤卢虹秀
Owner YULIN NORMAL UNIVERSITY
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