Phenylpiperazine compound and application thereof

A compound and alkyl technology, applied in the field of medicinal chemistry, can solve the problems of peripheral neurotoxicity, side effects, and side effects of chemotherapeutic agents, and achieve good tumor inhibitory activity and high safety effects

Pending Publication Date: 2022-05-27
JIANGSU CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these known radiosensitizers have unresolved issues, such as gastrointestinal dysfunction, peripheral neurotoxicity, and other side effect issues, and are rarely used in practice
[0004] Existing chemotherapeutic agents usually cause significant toxic side effects. Therefore, it is necessary to develop new radiosensitizers that can increase the efficacy of cancer radiotherapy, achieve therapeutic effects with lower radiation doses, and have clinically acceptable toxicity.

Method used

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  • Phenylpiperazine compound and application thereof
  • Phenylpiperazine compound and application thereof
  • Phenylpiperazine compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Preparation of 2-(4-(4-phenylpiperazin-1-yl)phenyl)-1H-indole

[0057]

[0058] Step 1 Preparation of Compound 1a

[0059]

[0060] 2-(4-Chlorophenyl)indole (286.8mg, 1.27mmol), piperazine (440.1mg, 4eq), cesium carbonate (620.0mg, 1.5eq) were dissolved in dimethyl sulfoxide (10mL), Stir overnight at room temperature. After monitoring the completion of the reaction, it was diluted with ethyl acetate, washed with saturated brine for 5 times, the organic phase was concentrated, and the compound 1a was isolated by column chromatography. ESI-MSm / z:[M+H] + = 278.1.

[0061] Step 2 Preparation of Compound 1

[0062]

[0063] Compound 1a (278.1 mg, 1 mmol), chlorobenzene (123.8 mg, 1.1 mmol) and cesium carbonate (488.7 mg, mmol) were dissolved in dimethyl sulfoxide (10 mL) and stirred at room temperature overnight. After monitoring the completion of the reaction, it was diluted with ethyl acetate, washed with saturated brine for 5 times, the organic pha...

Embodiment 2

[0064] Preparation of Example 2 Compound 2

[0065]

[0066] The preparation method is the same as the preparation method in Example 1, except that chlorobenzene is replaced by 4-chloropyridine to obtain the title compound. ESI-MS m / z:[M+H] + = 355.2.

Embodiment 3

[0067] Preparation of Example 3 Compound 3

[0068]

[0069] The preparation method is the same as that in Example 1, except that chlorobenzene is replaced by 3-chloropyridine to obtain the title compound. ESI-MS m / z:[M+H] + = 355.2.

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PUM

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Abstract

The invention relates to a phenylpiperazine compound and application thereof, in particular to a compound as shown in a formula (I), or pharmaceutically acceptable salt or stereoisomer thereof. Compared with independent application of radioactive rays or independent application of contrast compounds, the phenylpiperazine compound disclosed by the invention has the advantages that after the radioactive rays are applied, the combination disclosed by the invention has a remarkable curative effect in vivo, the state of rats is good, and the phenylpiperazine compound has relatively high safety;

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to phenylpiperazine compounds and applications thereof. Background technique [0002] Radiation therapy is a localized treatment of malignant tumors that involves the application of ionizing radiation as part of the treatment to control or kill malignant cells. The ionizing radiation damages the DNA of the exposed tissue and causes cell death, allowing normal organs and tissues to be destroyed. retention, so the number of patients treated by this method has grown rapidly, and it is estimated that about two-thirds of cancer patients receive radiotherapy. Radiation therapy treats many types of cancer and can also be used as part of adjuvant therapy to prevent tumors from coming back after surgery. Different types or sizes and states of cancer respond differently to radiation therapy: highly radiosensitive cancer cells such as leukemias, most lymphomas, and germ cell tumors are rapi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D403/12A61K41/00A61P35/00A61P35/02
CPCC07D401/12C07D403/12A61K41/0038A61P35/00A61P35/02
Inventor 吴俚蓉刘雅恬王丽君周佳伟宗丹顾佳佳燕丹何侠
Owner JIANGSU CANCER HOSPITAL
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