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Derivative of selenole and application of derivative

A technology of benzoselenodiazole and derivatives, which is applied in the field of chemical synthesis of drugs, can solve the problems of reproductive function impact, high toxicity and side effects, bone marrow suppression, etc., and achieve the effect of expanding the synthesis scale, reducing toxicity and side effects, and optimizing the process

Active Publication Date: 2018-03-13
JINAN UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because cancer cells divide and proliferate uncontrollably in the body, they are easily killed by this kind of chemotherapy drugs, but some tissues with vigorous cell division in the human body, such as hematopoietic tissue, hair follicle tissue, cells in the digestive tract and germ cells, are also Severely inhibited, resulting in severe toxic side effects such as bone marrow suppression, hair loss, nausea, vomiting, and reproductive function
In addition, most drugs are metabolized by the liver and excreted by the kidneys, and the drugs are highly toxic to the liver and kidneys.
Traditional chemotherapeutic drugs have low targeting and high toxic and side effects, which severely limit their application.

Method used

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  • Derivative of selenole and application of derivative
  • Derivative of selenole and application of derivative
  • Derivative of selenole and application of derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis and Characterization of 5-(2-Substituted Indolylbenzimidazole) Benzo[1,2,5]Selenadiazole Derivatives

[0039] (1) Weigh 30mmol of 3,3'-diaminobenzidine into a 1L flask, and fully dissolve it with 600ml of pure water (with an appropriate amount of HCl added). Weigh 30mmol selenium dioxide (SeO 2 ) was dissolved in 30mL hot water, and after dissolving, it was transferred to a constant pressure dropping funnel and slowly dropped into the flask. The reaction was stirred at room temperature for 1.5h. A large amount of yellow solids were precipitated. After the reaction was completed, suction filtration was performed. The filter residue was redissolved with sodium hydroxide solution to make it neutral, and the target product was obtained by suction filtration again. After drying, it was a reddish-brown solid powder with a yield of 95%.

[0040] (2) Weigh 3mmol of the product of step (1) (4-(benzo[c][1,2,5]selenadiazol-6-yl)benzene-1,2-diamino) in a 100mL flask, ad...

Embodiment 2

[0048] RGD-5-(2-substituted indolylbenzimidazole)benzo[1,2,5]selenadiazole RGD-SeD and SeD have antitumor activity and radiosensitization activity

[0049] In this example, the in vitro antitumor activity and radiosensitivity of SeD and RGD-SeD synthesized in Example 1 were evaluated by the MTT (thiazolium blue) method.

[0050] The human liver cancer cells HepG2 and human normal liver tissue L02 cells used in the experiment were respectively purchased from the American ATCC and the Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences. Cultured in DMEM medium (Gibco, Life technology) containing 10% FBS (Gibco, Life technology) in 5% CO 2 , 37°C cell culture incubator.

[0051] HepG2 and L02 cells were cultured to the logarithmic growth phase, digested with 0.25% trypsin (containing 0.02% EDTA), counted, and inoculated into 96-well plates, with 2000 cells per well, and the medium volume was 100 μL. Place in the incubator for 24 hours until the...

Embodiment 3

[0057] Cell uptake and localization of RGD-5-(2-substituted indolylbenzimidazole)benzo[1,2,5]selenadiazole

[0058] This example is to detect whether RGD-SeD improves its selective killing effect on tumor cells by increasing its uptake by tumor cells.

[0059] HepG2 and L02 cells were cultured to logarithmic growth phase, digested with 0.25% trypsin (containing 0.02% EDTA), counted, spread in 10cm culture dishes, each dish spread 1.5×10 6 cells. After the cells adhered to the wall, 50 μM (final concentration) of SeD or RGD-SeD were added respectively. Discard the medium at 0, 2, 4, and 8 hours, wash with PBS three times, digest with 0.25% trypsin, and collect the cells; mix with 5ml concentrated nitric acid:perchloric acid (volume ratio 3:1), and put in the nitration furnace Nitrate at 180°C for 2h, add 6mol / L hydrochloric acid for reduction for 30min, and finally detect the content of selenium with an atomic fluorescence spectrometer. Experimental results such as Figure ...

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Abstract

The invention discloses a selenole derivative structure and application thereof. According to the selenole derivative structure and the application thereof, selenadiazole with a tumor activity is modified, so that the utilization rate of an anti-tumor medicine is increased, and the toxic and side effect is reduced. Meanwhile, by use of the fluorescent property of an indole group, tumor cells and tissues are effectively imaged to realize diagnoses and treatment effects. The anti-tumor action of the selenadiazole is researched to find that the targeted selenadiazole is high in anti-tumor activity and can obviously improve the capacity of killing tumors by X-ray radiotherapy and NK immune cells, so that the selenadiazole has a wide application prospect. The raw materials of the selenole derivative structure are low in cost and easy to obtain, and the selenole derivative structure is high in product repetitiveness and stability.

Description

technical field [0001] The invention belongs to the field of chemically synthesized drugs, and in particular relates to the derivative structure and application of benzoselenadiazole. Background technique [0002] With the development of society, great changes have taken place in human living habits, eating patterns, travel patterns and other aspects. The potential fatal risks of cancer, cardiovascular disease, and epidemics have greatly increased. Human cancer morbidity and mortality have been increasing. Cancer has become the main health killer of all human beings except cardiovascular disease. Among most cancer treatment methods, tumor segment therapy is a comprehensive treatment strategy that combines therapy and diagnostic imaging, which can greatly improve the treatment efficiency of tumors. [Lohr J G, et al. Cancer cell. 2014,25:91-101.] Therefore, the development of cancer treatment strategies with tumor diagnosis and treatment has very important research signific...

Claims

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Application Information

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IPC IPC(8): C07D421/04C09K11/06A61K31/4178A61P35/00
CPCC07D421/04C09K11/06C09K2211/1029C09K2211/1044C09K2211/1055C09K2211/1074
Inventor 陈填烽曾德龙邓树林
Owner JINAN UNIVERSITY
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