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Antitumor application of small-molecule organic compound

A compound and anti-tumor drug technology, applied in the field of medicinal chemistry, can solve problems such as few structural types, low inhibition efficiency, and unclear mechanism of action

Active Publication Date: 2016-07-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In general, there are few structural types of IDO1 inhibitors, and most inhibitors still have defects such as low inhibition efficiency and unclear mechanism of action.

Method used

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  • Antitumor application of small-molecule organic compound
  • Antitumor application of small-molecule organic compound
  • Antitumor application of small-molecule organic compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Antitumor activity test of compound (I) (FN-01)

[0016] Compound FN-01 of the present invention has been carried out IDO1 inhibitory experiment, following is the pharmacological test and result of compound of the present invention:

[0017] IDO enzyme can catalyze the pyrrole epoxidation cleavage on tryptophan to produce N'-formylkynurenine. At room temperature, mix 40nM IDO enzyme and 900uM L-tryptophan, add reaction buffer (20mMascorbate, 3.5uMmethyleneblueand0.2mg / mLcatalasein50mMpotassiumphosphatebufferpH6.5), react at room temperature for three hours, and then The ultraviolet measurement is carried out on the instrument, and the detection wavelength is 321nm. The instrument reading is converted into: % activity = [(A-Ab) / (At-Ab)] × 100, and then use PrismGraphPadsofeware software to fit and calculate IC 50 value.

[0018] The test results are shown in Table 1:

[0019] Table 1. FN-01 inhibition test on IDO1

[0020] sample number

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Abstract

The invention relates to the field of medical chemistry, and in particular relates to an application of an organic small-molecule compound (I), which is discovered through virtual screening on the basis of bioinformatics and a computer aided design technology and is represented by FN-01, in preparation of an antitumor drug, and also relates to a pharmaceutical composition containing the type of compound.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to the application of a class of organic small molecule compounds represented by FN-01 in the preparation of antitumor drugs based on bioinformatics and computer-aided design technology through virtual screening, and the Pharmaceutical compositions of compounds. Background technique [0002] Indoleamine 2,3-dioxygenase (Indoleamine2,3-dioxygenase, IDO) is a heme-containing oxidoreductase, which is a monomeric enzyme and consists of 403 amino acid residues. Divided into two subtypes, namely IDO1 and IDO2. IDO is the only enzyme that can catalyze the metabolism of tryptophan outside the liver. It catalyzes the metabolism of tryptophan in the body through the kynurenine pathway, which is responsible for metabolizing more than 95% of tryptophan in the human body. IDO is the rate-limiting enzyme of the kynurenine pathway. [0003] Early clinical findings showed that trypt...

Claims

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Application Information

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IPC IPC(8): A61K31/5415A61P35/00
CPCA61K31/5415
Inventor 朱启华方升阳徐云根
Owner CHINA PHARM UNIV
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