HDAC and VEGFR dual-target inhibitor based on pazopanib structure and its preparation method and application

A pazopanib, dual-target technology, applied in the field of organic compound synthesis and pharmaceutical applications, can solve problems such as drug-drug interactions, unpredictable adverse reactions, and no related reports.

Active Publication Date: 2019-05-24
SHANDONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Clinically, the combined application of antineoplastic drugs with different mechanisms of action has been considered as a standard solution to avoid drug tolerance, but the following problems exist in the combined drug: (1) The pharmacokinetics of the combined drug is complex, drug-drug interactions, adverse The response is difficult to predict; (2) The compatibility and dosage setting of different drugs are clinically difficult
At present, there is no relevant report in the prior art on HDAC and VEGFR dual-target inhibitors based on the structure of pazopanib

Method used

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  • HDAC and VEGFR dual-target inhibitor based on pazopanib structure and its preparation method and application
  • HDAC and VEGFR dual-target inhibitor based on pazopanib structure and its preparation method and application
  • HDAC and VEGFR dual-target inhibitor based on pazopanib structure and its preparation method and application

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Embodiment Construction

[0175] The terms and definitions used in this document have the following meanings:

[0176] ACHN cells are human renal cell adenocarcinoma cells, AGS cells are human gastric adenocarcinoma cells, HEL cells are human erythroleukemia cells, HeLa cells are human cervical cancer cells, HT-1080 cells are human fibrosarcoma cells, HT-29 cells are human colon cancer cells, K562 The cells are human chronic myeloid leukemia cells, KG1 cells are human acute myeloid leukemia cells, MDA-MB-231 are human breast cancer cells, MOLT-4 are human acute lymphoblastic leukemia cells, PC-3 cells are human prostate cancer cells and HUVEC cells Umbilical vein endothelial cells.

[0177] 3. Application of HDAC and VEGFR dual-target inhibitors based on pazopanib structure

[0178] The present invention also provides the application of the HDAC and VEGFR dual-target inhibitor compound based on the structure of pazopanib in the preparation of drugs for preventing or treating tumor-related diseases.

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Abstract

The present invention relates to a pazopanib-based HDAC and VEGFR double-target inhibitor, a preparation method therefor and an application thereof. Said compound has a structure as presented in formula I, II or III. The present invention also relates to a preparation method for this type of compound and the application thereof in preparing drugs for treating or preventing oncological diseases.

Description

technical field [0001] The invention belongs to the technical field of organic compound synthesis and medical application, and specifically relates to a dual-target inhibitor of HDAC and VEGFR based on the structure of pazopanib and its preparation method and application. Background technique [0002] Pazopanib is a multi-target receptor tyrosine kinase inhibitor for the three subtypes of vascular endothelial growth factor receptor VEGFR (VEGFR-1, VEGFR-2, VEGFR-3) and associated receptors Body tyrosine kinases (PDGFRβ, c-Kit, FGF-R1, c-fms) all showed good inhibitory activity (IC 50 : 10, 30, 47, 84, 74, 140, 146 nM) (Harris, pHilip A. etc., Journal of Medicinal Chemistry 2008, 51, 4632). Pazopanib was approved by the US Food and Drug Administration FDA in October 2009 for the treatment of advanced renal cell carcinoma in patients with previous chemotherapy experience (Bukowski.etc., Nature Reviews Drug Discovery, 2010,9,17) , was approved by the FDA in April 2012 for the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/12A61K31/506A61P35/00A61P35/02
CPCA61K31/506A61P35/00A61P35/02C07D239/48C07D403/12
Inventor 张颖杰徐文方臧杰
Owner SHANDONG UNIV
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