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

Compound applicable to preparing chemotherapeutic drugs

A chemotherapeutic drug and compound technology, applied in drug combination, organic chemistry, antineoplastic drugs, etc., can solve the problems of not prolonging the survival of patients with squamous cell carcinoma and prolonging the survival of patients with advanced squamous cell carcinoma

Inactive Publication Date: 2014-06-04
张晓凤
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the past, the combination chemotherapy of cisplatin (Cisplain, DDP) and 5-fluorouracil (5-fluorouracil, 5-FU) was mostly used in the chemotherapy of squamous cell carcinoma, the effective rate was 25%-35%, and the median survival time was 6-9 months. The main side effects are mucositis and myelosuppression, but there is no evidence-based medical evidence to prove that chemotherapy can prolong the survival of patients with advanced squamous cell carcinoma
2006 Homs et al (Homs MYV, v. d. Gaast A, Siersema PD, et al . 2006) published a meta-analysis of advanced squamous cell carcinoma chemotherapy, collected 7 randomized controlled clinical trials, and the results showed that chemotherapy based on DDP combined with 5-FU could not prolong the survival of patients with squamous cell carcinoma

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
  • Compound applicable to preparing chemotherapeutic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1: the preparation of formula I compound:

[0012] (1) Synthesis of (E)-4-(4-hydroxyphenyl)-3-buten-2-one

[0013] Add 4-hydroxybenzaldehyde (20.0 mmol), 24 mL of acetone, and 10 mL of water to a 100 mL three-necked flask in sequence, stir until all the solids are dissolved, then add a solution of sodium hydroxide (24 mmol)+20 mL of water dropwise, The reaction liquid changed from light yellow clear liquid to wine red clear liquid, and the reaction was complete. Acetone was removed by rotary evaporation, and 70 mL of hot water was added to the residual liquid until the red solid was completely dissolved. Carbon dioxide was introduced for about 30 minutes until the reaction liquid no longer changed color. , a light yellow solid is produced, filtered, washed with water, dried, and recrystallized with acetone / water to obtain a light yellow solid, yield: 84%,

[0014] Melting point: 99~101 °C.

[0015] (2) Synthesis of (1E,4E)-1-(4-hydroxyphenyl)-5-(3-mercaptom...

Embodiment 2

[0024] Embodiment 2: Drug efficacy test:

[0025] Table 1 lists the cell lines used in the test

[0026] Table 1 Cell lines used in the test

[0027] cell line source Histological source and type KB ATCC Oral Squamous Carcinoma HELA ATCC Cervical Squamous Carcinoma NIH-3T3 (Normal) ATCC mouse embryonic fibroblasts

[0028] *ATCC: American Type Culture Collection

[0029] The sulforhodamine B protein staining method was used to detect the inhibitory effect of drugs on the proliferation and growth of squamous cell carcinoma cells. The main steps are as follows:

[0030] According to the cell growth rate (doubling time) determined in the preliminary experiment, a certain number of logarithmic growth phase cells were inoculated in a 96-well culture plate (90 μl / well). After growing for 24 hours, different concentrations of the compound of formula I and its crystal form were added under the condition of darkening. Simultaneously set...

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

PropertyMeasurementUnit
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention provides a compound disclosed as Formula I and a crystal thereof. The compound can be used for preparing drugs for chemotherapy of squamous carcinoma, including oral squamous carcinoma, cervix squamous carcinoma or gullet squamous carcinoma. I.

Description

technical field [0001] The present invention relates to a compound which can be used as chemotherapeutic agent and its preparation method. Background technique [0002] Squamous cell carcinoma (squamous cell carcinoma) is referred to as squamous cell carcinoma, which often occurs in parts of the body covered by squamous epithelium, such as skin, mouth, lips, cervix, vagina, esophagus, and throat. Some parts, such as bronchi, gallbladder, kidney, etc., are not covered by squamous epithelium normally, but squamous cell carcinoma can occur through squamous metaplasia. This cancer is often cauliflower-shaped to the naked eye, and can also form ulcers due to necrosis and shedding of cancer tissue. At the same time, the cancer tissue also grows invasively to the deep layer. [0003] Squamous cell carcinoma is a malignant tumor of the epidermal cells of the skin. The incidence rate is about 8% of eyelid malignancies. More common in the elderly over the age of 50. Men outnumber...

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 Applications(China)
IPC IPC(8): C07C323/47A61K31/15A61P35/00
Inventor 张晓凤
Owner 张晓凤
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com