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

Methionyl aminopeptidase inhibitor

A technology of methionyl aminopeptidase and thionyl aminopeptidase, which is applied in the field of a class of methionyl aminopeptidase inhibitors, can solve problems such as failure to achieve satisfactory results in life and health treatment, and achieve high Inhibiting activity, simple structure, and easy preparation

Inactive Publication Date: 2007-12-26
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In recent years, cancer chemotherapy has made considerable progress, and the survival time of cancer patients has been significantly prolonged. In particular, breakthroughs have been made in the treatment of leukemia and malignant lymphoma. Treatment of solid tumors fails to achieve satisfactory results

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
  • Methionyl aminopeptidase inhibitor
  • Methionyl aminopeptidase inhibitor
  • Methionyl aminopeptidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0038] The present invention will be further described below in conjunction with specific embodiments, but the present invention is not limited.

[0039] 1 H-NMR was measured with Varian MercuryAMX300 instrument; MS was measured with VG ZAB-HS or VG-7070 instrument, except for the EI source (70ev); all solvents were re-distilled before use. The water solvents are all obtained by drying according to standard methods; except for the instructions, all reactions are carried out under the protection of Ar gas and followed by TLC. The post-treatments are all washed with saturated brine and anhydrous MgSO 4 Drying process; except for instructions, the purification of the product uses silica gel (200-300 mesh) column chromatography; the silica gel used includes 200-300 mesh and GF 254 Produced by Qingdao Ocean Chemical Plant or Yantai Yuanbo Silicone Company.

[0040] 1. Preparation of compound 6

[0041]

[0042] Dissolve o-nitrobenzoyl chloride (5mmol) in dichloromethane (15ml), add 2...

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

One kind of heterocyclic compounds is designed and synthesized as novel methionyl aminopeptidase inhibitor.

Description

Technical field [0001] The small molecule organic compounds involved in the present invention show high inhibitory activity on methionyl aminopeptidase (MetAPs), and show certain selectivity for different MetAPs subtypes, so it can be used as a new class of anti-methionyl aminopeptidase (MetAPs). Leading compound for tumor and antibacterial drug research. Background technique [0002] The translation of all proteins in the cytoplasm of prokaryotic cells starts from the N-terminal methionine, but the translation of proteins in eukaryotic cells, mitochondria and chloroplasts starts from N-formylated methionine, which is formylated The group is generally removed by the deformylase in the process of accompanying translation. Whether in eukaryotic cells or prokaryotic cells, methionyl aminopeptidase (MetAPs) selectively cuts off the N-terminal methionine of nascent proteins or polypeptide chains. The excision of the N-terminal methionine of the nascent protein or polypeptide chain pla...

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): C07D277/44C07D263/48C07D233/88A61K31/426A61K31/421A61P35/00A61P31/00C07D277/22C07D277/38C07D277/46C07D417/12
CPCC07D277/46C07D417/12A61P31/00A61P35/00
Inventor 南发俊叶其壮刘志英李静雅
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI