High-activity tacrine-platinum (II) complexes and synthesis method and application thereof

A synthesis method and complex technology, applied in the field of medicine, can solve the problems such as the synthesis method and application of platinum (II) complexes that have not yet been seen, and achieve the effects of superior in vitro antitumor activity, significant inhibitory effect, and good medicinal value.

Active Publication Date: 2018-01-26
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From structural analysis, its parent ring structure has better aromatic planarity, is a kind of excellent organic ligand; And

Method used

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  • High-activity tacrine-platinum (II) complexes and synthesis method and application thereof
  • High-activity tacrine-platinum (II) complexes and synthesis method and application thereof
  • High-activity tacrine-platinum (II) complexes and synthesis method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0067] Example 1

[0068] Weigh accurately 1.0mmol of 1.0mmol of dichlorobis(dimethylsulfoxide)platinum(II) and HL, dissolve HL in 42mL of methanol, add dichlorobis(dimethylsulfoxide) Sulfone) platinum (II) was dissolved in 3 mL of dimethyl sulfoxide solution, the two solutions were mixed, reacted at 55°C for 12 hours, concentrated and evaporated to remove 55% of the solvent, cooled to room temperature and stood still, and a yellow solid precipitated , Suction filtration, the solid was washed with water, methanol, and ether successively, the solid was separated, and the target complex 1 was obtained after vacuum drying (yield 97.3%).

[0069] Identify the obtained yellow massive crystals:

[0070] (1) Infrared spectrum, the spectrum is as Figure 4 Shown.

[0071] IR(KBr): 3886,3783,3437,3397,2927,2382,1611,1552,1493,1443,1415,1118,1021,977,777,687,592,441cm -1 .

[0072] (2) The proton nuclear magnetic resonance spectrum, the spectrum is as follows Figure 5 Shown.

[0073] 1 H NMR(60...

Example Embodiment

[0082] Example 2

[0083] Weigh each 1 mmol of complex 1 and 4,4'-dimethyl-2,2'-bipyridine, dissolve them in 65 mL of ethanol, react at 55°C for 24 hours, concentrate and evaporate to remove 50% of the solvent. After cooling to room temperature and standing still, a red-brown solid was precipitated, and the solid was separated, washed with water, methanol, and ether in turn, and dried to obtain a red-brown solid product (yield 91.6%).

[0084] Identify the obtained red-brown product:

[0085] (1) Infrared spectrum, the spectrum is as Picture 9 Shown.

[0086] IR (KBr): 3781, 3694, 3411, 2928, 2860, 1614, 1552, 1493, 1444, 1414, 1170, 1122, 924, 520cm -1 .

[0087] (2) The proton nuclear magnetic resonance spectrum, the spectrum is as follows Picture 10 Shown.

[0088] 1 H NMR(600MHz, DMSO-d 6 )δ9.26(d,J=5.2Hz,1H), 9.19(d,J=6.0Hz,2H), 9.11(d,J=4.9Hz,1H), 8.39(s,1H), 7.53(d, J = 5.2Hz, 1H), 7.37 (t, J = 7.7 Hz, 1H), 7.14-7.02 (m, 2H), 2.79 (s, 2H), 2.54 (s, 2H), 2.52 (s, 3H), 2.46 (s,...

Example Embodiment

[0094] Example 3

[0095] Accurately weigh the 1.0mmol complex 1 and 1.0mmol 4,7-diphenyl-1,10-phenanthroline, and dissolve them in 35mL of 80v / v% methanol and acetonitrile (methanol and acetonitrile) The volume ratio is 4:1) In the mixed solution, react at 80°C for 36 hours, concentrate and evaporate to remove 45% of the solvent, cool to room temperature and stand still, suction and filter, the solid is washed with water, methanol, ether, and dried. , A black solid target product was obtained (yield 86.3%).

[0096] Identify the resulting black product:

[0097] (1) Infrared spectrum, the spectrum is as Picture 12 Shown.

[0098] IR(KBr): 3957,3783,3696,3634,3429,2932,2379,1607,1557,1494,1420,1154,909,768,706,617,524cm -1 .

[0099] (2) The proton nuclear magnetic resonance spectrum, the spectrum is as follows Figure 13 Shown.

[0100] 1 H NMR(500MHz, DMSO-d 6 )δ11.58(s,1H),9.72(s,1H),9.49(s,1H),9.37(s,1H),7.88(d,J=2.9Hz,2H),7.86(d,J=3.7 Hz, 1H), 7.71 (s, 6H), 7.71 (s, 2H), 7.65 (s...

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Abstract

The invention discloses high-activity tacrine-platinum (II) complexes and a synthesis method and application thereof, and relates to the technical field of medicine. The purpose of the invention is toprovide six high-activity tacrine-platinum (II) complexes having novel structures. The six high-activity tacrine-platinum (II) complexes have chemical structural formulas shown in the formulas 1 to 6. The high-activity tacrine-platinum (II) complexes can be used for preparation of antitumor drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a highly active tacrine-platinum (II) complex and its synthesis method and application. Background technique [0002] In 1978, the FDA approved cisplatin as the first generation metal platinum antitumor drug for clinical use (Rosenberg, B.; et al. Nature, 1965, 205:698-699.), but its use was limited due to severe side effects. clinical application. With the development of economy and the change of lifestyle, the prevalence of cancer is getting higher and higher, seriously threatening human life and health. Although the currently synthesized platinum-based antineoplastic drugs have some anti-tumor activity, there are few drugs with better efficacy than cisplatin. Therefore, the design and development of platinum-based antineoplastic drugs need to be innovated on the basis of traditional ideas and breakthrough. [0003] In addition, tacrine is the first acetylcholinesterase inh...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
Inventor 覃其品谭明雄王书龙罗旭健
Owner YULIN NORMAL UNIVERSITY
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