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Novel regorafenib anti-tumor platinum (II) complex and preparation method and application thereof

An anti-tumor and complex technology, applied in the field of novel regorafenib anti-tumor platinum complex and its preparation, to achieve the effect of superior in vitro anti-tumor activity

Active Publication Date: 2018-12-14
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 are no related reports on complexes and anti-tumor activity studies using them as active ligands. In order to expand the clinical application of this drug, this study uses Regorafenib as the active ligand Ligand synthesis targeting human lung cancer drug-resistant cells (A549 / DDP) anti-tumor platinum complex, and its anti-tumor activity and application were studied

Method used

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  • Novel regorafenib anti-tumor platinum (II) complex and preparation method and application thereof
  • Novel regorafenib anti-tumor platinum (II) complex and preparation method and application thereof
  • Novel regorafenib anti-tumor platinum (II) complex and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Add 1.0 mmol ligand RFB and 1.0 mmol cis-PtCl in a 50 mL autoclave 2 (DMSO) 2 , add 25.0mL of anhydrous methanol and 1.0mL of distilled water, heat at 55°C for 36 hours, cool down to room temperature, a large amount of yellow product precipitates, filter with suction, wash the yellow product with methanol, acetone and ether in turn, 45 After vacuum drying at °C, a yellow product was finally obtained with a yield of 95.0%.

[0027] The resulting yellow product is identified:

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

[0029] IR(KBr):3644,3341,3054,3006,2921,1696,1614,1490,1458,1423,1317,1197,1159,1140,1031,971,884,838,732,701,663,565,531,446cm -1 .

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

[0031] ESI-MS m / z:902.1[M-H+DMSO] - , where M is its molecular weight.

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

[0033] 1 H NMR (400MHz, DMSO-d 6 )δ9.56(s,1H),9.43(d,J=6.7Hz,1...

Embodiment 2

[0042] Add ligand 1.0mmol RFB and 5.0mmol cis-PtCl in a 50mL autoclave2 (DMSO) 2 , add 35.0 mL of absolute ethanol and 10.0 mL of distilled water, heat at 80°C for 48 hours, cool down to room temperature, a large amount of yellow product precipitates, filter with suction, wash the yellow product with methanol, acetone and diethyl ether successively, 45 After vacuum drying at °C, complex 1 was finally obtained with a yield of 80.0%.

Embodiment 3

[0044] Add ligand 5.0mmol RFB and 1.0mmol cis-PtCl in a 50mL autoclave 2 (DMSO) 2 , add 5.0mL of acetonitrile and 30.0mL of distilled water, heat at 45°C for 8 hours, cool down to room temperature, a large amount of yellow product precipitates, filter with suction, wash the yellow product with methanol, acetone and diethyl ether in turn, at 45°C After vacuum drying, complex 1 was finally obtained with a yield of 85.0%.

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Abstract

The invention discloses a novel regorafenib anti-tumor platinum (II) complex. A chemical structural formula of the platinum (II) complex is as shown in the specification. The platinum (II) complex expresses excellent anti-tumor activity in vitro, has a potential medicinal value and is hopefully used for preparing various anti-tumor drugs. The invention further discloses a preparation method and the application of the platinum (II) complex.

Description

technical field [0001] The invention relates to the field of regorafenib anti-tumor drugs and their preparation, in particular to a novel regorafenib anti-tumor platinum (II) complex and its preparation method and application. Background technique [0002] Since 1969, American chemist Bosenberg B. et al first discovered cis-dichlorodiammine platinum (II), which has strong anti-tumor activity in animals, and inorganic metal complexes have become a new class of anticancer drugs. The research has aroused great attention of chemists. Although the currently widely used metal complex anticancer drugs are only metal drugs such as cisplatin, carboplatin, nedaplatin, and oxaliplatin, research in this field has shown that more drugs have high anticancer activity and low toxicity and side effects. The anti-cancer drugs of metal complexes are expected to enter clinical trials, so that there is a greater range of choices for cancer chemotherapy. Because cisplatin drugs have serious sid...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00A61K31/555
CPCA61P35/00C07F15/0086
Inventor 覃其品谭明雄王书龙王振凤罗冬妹韦庆敏陆克李秋焰
Owner YULIN NORMAL UNIVERSITY
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