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Polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof and application of polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof

A technology of polyarylethylene and compounds, applied in organic chemistry, antineoplastic drugs, drug combinations, etc., can solve problems such as no breakthroughs, achieve the effects of inhibiting the repair process, improving the effect of radiotherapy, and improving the effect of radiotherapy

Pending Publication Date: 2022-03-04
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still no breakthrough in targeted drugs, and the discovery of radiosensitizing drugs that can overcome these factors has an urgent clinical need

Method used

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  • Polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof and application of polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof
  • Polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof and application of polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof
  • Polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof and application of polyaromatic ethylene beta-diketone compound or pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Example β- more than one vinyl aromatic diketones PT33-F, PT33-Cl, PT33-I, PTDO-F, PTDO-Cl, PTDO-Br, Synthesis and characterization of PTDO-I

[0077] Polyaromatic vinyl β- diketones PT33-F, PT33-Cl, PT33-I, PTDO-F, synthetic PTDO-Cl, PTDO-Br, PTDO-I is performed according to the following reaction scheme:

[0078]

[0079] Specifically: in 100mL round-bottomed flask, boron anhydride (0.35g, 5mmol, 1.0eq), acetylacetone (1g, 10mmoL, 2eq) was dissolved in 10mL of ethyl acetate, 70 deg.] C reaction 3h. The solvent was removed by suction filtration, washed twice with cyclohexane, as a white solid. In 100mL round-bottomed flask, as a white solid, corresponding aromatic aldehyde I (20mmoL, 4eq), butyl borate (4.60g, 20mmol, 4.0eq) was dissolved in 20mL ethyl acetate and stirred for 30min 70 ℃. N-butylamine (73mg, 1mmol, 0.2eq) was diluted with 5mL of ethyl acetate, a dropping funnel was added dropwise to the reaction mixture was slowly heated to 85 ℃, the reaction was continue...

Embodiment 2

[0088] Example 2 Formula (1) compound radiotherapy representative tumor cell sensitizing activity shown

[0089] Selecting a representative tumor cell lines of each system, reproductive system tumors include ① containing cervical carcinoma (SW756), endometrial carcinoma (ESS-1), ovarian cancer (OVCAR-5) and prostate (PC-3) cell line; ② tumors including gastric digestive system (AGS), liver cancer (Huh-7), in colorectal cancer (HCTl 16) and pancreatic cancer (PANC1) cell line; ③ nasopharyngeal tumors, including respiratory system (CNE2), hypopharynx (FaDu) and lung cancer (of A549) cell lines; ④ nervous system tumors include astrocytomas (U87), neuroblastoma (ACN) and medulloblastoma (PFSK-1) cell line; ⑤ urinary system tumors including renal cell carcinoma (A704) and bladder cancer (T24) cell line; ⑥ skin cancers include squamous cell carcinoma (of A431), and melanoma (COLO-829) cell line; ⑦ bone and soft tissue sarcomas include osteosarcoma (U20S), and soft tissue sarcomas (HT -1...

Embodiment 3

[0094] Example 3PT33 cell sensitizing activity in different tumor models embodiment

[0095] Characterization of Effects of drugs combined with radiation therapy and colony formation on plates using cloning experiments. The HCT116 and SW837 cells at a density of 1000 cells / well were seeded into 6 well plates, respectively, under normoxic and hypoxic state (5v / v% O 2 )nourish. After 24 hours, treated with X-rays and / or different concentrations of the drug dose specified cells, and then cultured for 10-14 days, then fixed with methanol, stained with crystal violet 0.5%. Collection of cells containing 50 or more colonies were counted, the sensitizer compound with the ability to reduce the front with a multiple cloning cell FC represents, as a result figure 1 Indicated.

[0096] figure 1 The results showed that, PT33 is effective in enhancing the effect of radiotherapy of various tumor cell lines, and under hypoxic conditions, which is further enhanced sensitizing activity.

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Abstract

The invention discloses a polyarylethylenebeta-diketone compound or a pharmaceutically acceptable salt thereof and an application of the polyarylethylenebeta-diketone compound or the pharmaceutically acceptable salt thereof. The polyarylethylenebeta-diketone compound provided by the invention has a radiotherapy sensitization effect, and the radiotherapy effect on various tumors can be remarkably improved at a low dosage; a stronger sensibilization effect is shown on low-oxygen environment tumors; the repair process after DNA damage caused by radiotherapy can be effectively inhibited, and an interferon gene activation protein (STING) signal channel can be effectively and synergistically activated. Therefore, when the polyarylethylenebeta-diketone compound provided by the invention is applied to tumor radiotherapy as a radiotherapy sensitization active component, the tumor radiotherapy effect can be greatly improved.

Description

Technical field [0001] The present invention belongs to the field of drug technology, and more relates to a polyary ethylene β-diketone compound or a pharmaceutically acceptable salt thereof. Background technique [0002] Radiotherapy is one of the important ways of malignant tumors, and new adjuvant treatment based on conventional long-range radiotherapy has become a standard plan for the treatment of various malignant tumors. However, long-term clinical studies have found that malignant tumor patients have different degrees of response to radioactive treatment, although some patients can achieve pathological remission at the end of the treatment cycle, however, some patients cannot benefit from long-range treatment, small part Patients even have deteriorated progress. As Zhongshan University Tumor Prevention Center, the Governoracic Department has shown (2014-2019, the annual annual charge of 1800 cases) shows that patients who cannot benefit from 30%, and the proportion of pro...

Claims

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Application Information

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IPC IPC(8): C07D317/64C07C49/255A61P35/00
CPCC07D317/64C07C49/255A61P35/00
Inventor 卜宪章岳欣徐慧莹伍伟健
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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