Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of schizocommunin derivative and its preparation method and application

A technology of derivatives and compounds, applied in the field of schizocommunin derivatives and their preparation, can solve problems such as toxic side effects or drug resistance, and achieve significant inhibitory effects, strong binding and stabilizing capabilities, and broad application space

Active Publication Date: 2020-04-24
SUN YAT SEN UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such traditional chemotherapy drugs targeting double-helix DNA can also cause severe toxic side effects or drug resistance

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of schizocommunin derivative and its preparation method and application
  • A kind of schizocommunin derivative and its preparation method and application
  • A kind of schizocommunin derivative and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: the synthesis of compound Q1-1

[0046]

[0047] Add 2-amino-4-fluorobenzoic acid (5g, 32mmol) and 10mL acetic anhydride into a 100mL round-bottomed flask, heat to reflux for 3h, add the reaction system dropwise to 200mL ice water, filter with suction, and wash with water 3 times to obtain the compound I-1, yield 91%.

Embodiment 2

[0048] Embodiment 2: the synthesis of compound Q1-2

[0049]

[0050] The method is the same as in Example 1, except that 2-amino-4,5-difluorobenzoic acid is used instead of 2-amino-4-fluorobenzoic acid to obtain a white solid with a yield of 80%.

Embodiment 3

[0051] Embodiment 3: the synthesis of compound Q2-1

[0052]

[0053] Take compound Q1-1 (1.78g, 10mmol), add 10mL of 25% concentrated ammonia water into a 100mL round bottom flask, heat to reflux for 2h, cool, filter with suction, and wash with water 3 times to obtain a white solid with a yield of 89%. 1 H NMR (400MHz, DMSO-d 6 )δ12.03(s,1H),8.13(dd,J=8.7,6.4Hz,1H),7.66–7.04(m,2H),2.35(s,3H).

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the field of medicinal chemistry, and particularly relates to a schizocommunin derivative and a preparation method and application thereof. The structural formula of the schizocommunin derivative is shown in the description, wherein R1 and R3 are hydrogen or fluorine atoms, R2 is amidogen or substituted amidogen or a five-membered or six-membered heterocycle group, R4 is ahydrogen atom or amidogen or substituted amidogen or a five-membered or six-membered heterocycle group, R5 is a hydrogen atom or amidogen or substituted amidogen or halohydrocarbon or a five-memberedor six-membered heterocycle group, and R6 is a hydrogen atom or an alkyl group; a substituent group is amidogen or a five-membered or six-membered heterocycle group. The schizocommunin derivative hasextremely high binding and stabilizing capacities for telomere DNA which is rich in guanine, has a significant anti-cancer effect, and can be used for preparing anti-cancer drugs which have selectivity. Further experiments show that the schizocommunin derivative has significant inhibition effects on various cancer cell lines and has broad application space in anti-cancer drug preparation.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and more specifically relates to a schizocommunin derivative and its preparation method and application. Background technique [0002] Malignant tumor is a major disease that endangers human health and life safety. According to the statistics of the World Health Organization (WHO), there are as many as 90.5 million malignant tumor patients worldwide, and there are 14.1 million new cases every year. 8.8 million people die of cancer every year, and nearly 2 million people die of cancer every year in China. The research and development of anticancer drugs has always been a hot spot for medicinal chemists. Finding highly efficient and highly selective anticancer drugs is one of the important directions of drug development. [0003] Chemotherapy is an important method to treat cancer, among which the more classic and widely used chemotherapy drugs target double-helix DNA or regulate DNA replicatio...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/06A61K31/517A61K31/5377A61P35/00A61P35/02
Inventor 黄志纾谭嘉恒车通
Owner SUN YAT SEN UNIV