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Palladium complexes of 2-benzoylpyridine thiosemicarbazone and synthesis method thereof

A technology of benzoylpyridine thiosemicarbazide and benzoylpyridine, which is applied in the field of palladium complexes with 2-benzoylpyridine thiosemicarbazide and synthesis thereof, can solve problems and accelerate the exploration and development of alternative therapy And other issues

Active Publication Date: 2020-01-21
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, extensive studies conducted over the past few decades have provided indisputable evidence for the adverse side effects of cisplatin and other platinum-based anticancer drugs such as carboplatin and oxaliplatin, accelerating the exploration and development of alternative therapies

Method used

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  • Palladium complexes of 2-benzoylpyridine thiosemicarbazone and synthesis method thereof
  • Palladium complexes of 2-benzoylpyridine thiosemicarbazone and synthesis method thereof
  • Palladium complexes of 2-benzoylpyridine thiosemicarbazone and synthesis method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The synthesis of palladium complex C1 comprises the following steps:

[0026] (1) Mix 3mmol of 2-benzoylpyridine and 3mmol of 4,4-dimethyl-3-thiosemicarbazide, dissolve in 20ml of methanol after mixing, add 500ul of concentrated sulfuric acid dropwise, and stir under reflux at 65°C After reacting for 6 hours, a light yellow precipitate was obtained; the precipitate was filtered, washed with saturated sodium bicarbonate and water successively, and the eluent was petroleum ether:ethyl acetate=10:1, and after drying, the ligand L1 was obtained. Rate: 82%;

[0027] Elemental analysis, Anal.Calcd(%) for C 15 h 16 N 4 S:C,63.35;H,5,67;N,19.70;S,11.28.Found:C,63.28;H,5.11;N,18.75;S,11.14;

[0028] Infrared spectrum, IR, cm -1 :3463(s,amide),3274(s,NH),3208(m,aromatic hydrogen),1526(s),1495(s),1463(s,aromatic),1287(m,C=N),1079 (s, thioamide), 934 (m, C-H), 757 (m, C=S), 694 (m);

[0029] Mass Spectrum, ESI+m / z:C 15 h 16 N 4 S,284.11[M+H] + ;

[0030] (2) Weigh 0.05m...

Embodiment 2

[0035] The synthesis of palladium complex C2 comprises the following steps:

[0036] (1) Mix 3mmol of 2-benzoylpyridine and 3mmol of 3-pyrrole-3-thiosemicarbazide, dissolve in 20ml of methanol after mixing, add 500uL of concentrated sulfuric acid dropwise, and reflux and stir at 65°C for 6h. A light yellow precipitate was obtained; the precipitate was filtered, washed with saturated sodium bicarbonate and water successively after filtration, separated by silica gel column chromatography, and the eluent was petroleum ether:ethyl acetate=10:1, and the ligand L2 was obtained after drying , Yield: 85%;

[0037] Elemental analysis, Anal.Calcd(%) for C 17 h 18 N 4 S: C, 65.78; H, 5.84; N, 18.05; S, 10.33. Found: C, 65.55; H, 5.59; N, 18.27; S, 10.04;

[0038] Infrared spectrum, IR, cm -1 :3355(s,amide),3249(s,NH),3057(m,aromatic hydrogen),1585(s),1469(s),1438(s,aromatic),1236(m,C=N),1154 (s, thioamide), 895 (m, C-H), 797 (m, C=S), 695 (m);

[0039] Mass Spectrum, ESI+m / z:C 1...

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Abstract

The invention discloses palladium complexes of 2-benzoylpyridine thiosemicarbazone and a synthesis method of the palladium complexes. The method comprises the following steps: respectively mixing andreacting 2-benzoylpyridine with 4,4-dimethyl-3-thiosemicarbazone and 3-pyrrole-3-thiosemicarbazone to prepare a ligand; and reacting the prepared ligand with PdCl2 to obtain the palladium complexes C1and C2. In-vitro proliferation inhibition activity experiments are further carried out on the synthesized palladium complexes C1-C2, and the results show that the synthesized palladium complexes havegenerally good in-vitro activity, show good inhibition activity, have little toxic effect on human normal cells, and are suitable for preparing high-efficiency and low-toxicity anti-tumor drugs.

Description

technical field [0001] The invention relates to a palladium complex, in particular to a palladium complex with 2-benzoylpyridine thiosemicarbazone and a synthesis method thereof. Background technique [0002] Since its introduction in medical practice in the 1970s, cisplatin has been a driving force in the design of platinum-like drugs to treat cancer. However, extensive studies conducted in the past decades have provided indisputable evidence for the adverse side effects of cisplatin and other platinum-based anticancer drugs such as carboplatin and oxaliplatin, accelerating the exploration and development of alternative therapies. [0003] In recent years, due to the similar coordination chemical properties of palladium (II) complexes and platinum (II), it is attempted to develop new anti-tumor drugs based on this, so as to replace platinum anti-tumor drugs. Platinum has good anticancer and apoptosis-inducing activities in vitro, and has low toxicity to normal cells. [0...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0066
Inventor 杨峰李文娟庞金惠贾晓颖
Owner GUANGXI NORMAL UNIV
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