Preparation method and application of CDK4

A compound and general formula technology, applied in the field of preparation of tetrahydro-β-carboline compounds, can solve problems such as poor activity

Inactive Publication Date: 2019-03-12
LANZHOU UNIVERSITY
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  • Abstract
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  • Claims
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Problems solved by technology

However, it can also be observed that fascaplysin is less active against other CDKs, the IC of CDK1 / Cyclin B 50 >100 μM, IC for CDK2 / Cyclin A and CDK-2 / Cyclin E 50 >50 μM, IC of CDK5 / p35 50 20μM

Method used

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  • Preparation method and application of CDK4
  • Preparation method and application of CDK4
  • Preparation method and application of CDK4

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Embodiment Construction

[0023] The present invention will be explained in detail below in conjunction with the examples of compound preparation and pharmacological experiments.

[0024] 1. Compound Preparation

[0025] 1) Preparation of compound of general formula (I) Preparation of compound

[0026] a: Dissolve 6.00g of tryptamine in 100mL of water, add concentrated hydrochloric acid drop by drop until the solid is completely dissolved, add 4 equivalents of glyoxylic acid and 10% KOH solution dropwise at room temperature and constant pressure to adjust the pH to about 3-4. React at room temperature for 4 hours until the solid precipitates completely, monitor by thin layer chromatography until the reaction is complete, filter with suction, wash the filter cake with water three times, and recrystallize with methanol to obtain the intermediate 1,2,3,4-tetrahydro-β-carboline-1-carboxylate Acid 7.05g.

[0027] b: Dissolve 2.4mmol (0.5g) of benzoic acid with different substituents in 5ml of dry THF, add...

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Abstract

The invention relates to compounds shown as general formulas (I) and (II), pharmacologically acceptable salt thereof and a preparation method and application thereof. The compounds and the salt can beused for preparing drug for preventing or treating diseases related to a cyclin-dependent kinase (CDK4) inhibitor and drug for treating melanoma, liver cancer, stomach cancer, non-small cell lung cancer, prostatic cancer, thyroid cancer, colorectal cancer, pancreatic cancer, ovarian cancer, breast cancer, esophagus cancer and gastrointestinal cancer.

Description

technical field [0001] The present invention relates to a kind of pharmaceutical compound, especially a kind of preparation method and application of tetrahydro-β-carboline compound. Background technique [0002] Fascaplysin is a red pigment, which was first isolated from the Fiji marine sponge Fascaplysinopsis sp by Roll et al. in 1988. It is also the first naturally occurring five-ring ring system 12H-pyrido[1,2-a: 3, 4-b] Diindole members. Fascaplysin exhibits a wide range of biological activities, including antibacterial, antifungal, antiviral, HIV-1-RT, p56 tyrosine kinase, antimalarial, also effective against many cancer cell lines, and CDK4 inhibition. Fascaplysin can inhibit the growth of several microorganisms, including Staphylococcus aureus, Escherichia coli, Candida albicans and Saccharomyces cerevisiae. fascaplysin shows inhibition of proliferation of mouse leukemia cells L-1210, ED 50 The value was 0.2 μM / mL and showed selectivity in the murine tumor cytotox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61P35/00
CPCA61P35/00C07D471/04
Inventor 贺殿唐磊朱红甜胡春红
Owner LANZHOU UNIVERSITY
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