2,4-diarylaminopyrimidine derivatives containing hydroxamic acid fragments and their preparation and application

A technology of diarylaminopyrimidine and hydroxamic acid, applied in the field of 2,4-diarylaminopyrimidine derivatives and its preparation
CN105646371BInactive Publication Date: 2019-10-01ZHEJIANG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG UNIV
Publication Date
2019-10-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides 2,4-diarylamine pyrimidine derivatives containing hydroxamic acid fragments shown in formulas I and II. 2,4-diarylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the remarkable anti-proliferative effect is achieved for tumor cells (a human lung adenocarcinoma cell line H1975 and an overexpression EGFR human epidermal carcinoma cell line A431) related to EGFR tyrosine kinase activity on the cellular level, and a human cervical carcinoma cell line Hela, a human oral epidermoid carcinoma cell line KB, a human promyelocytic acute leukemia cell line HL60, a human hepatoma cell line HepG2, a human colon cancer cell line SW620 and other tumor cells related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.
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Description

technical field

[0001] The invention belongs to the field of pharmacy, and relates to a 2,4-diarylaminopyrimidine derivative containing a hydroxamic acid fragment, a preparation method and application thereof. Background technique

[0002] Studies have found that one or more EGFR family receptors are mutated or overexpressed in more than 60% of malignant tumors. Tyrosine kinases play an important regulatory role in the process of cell growth, proliferation and apoptosis. Small-molecule EGFR tyrosine kinase inhibitors compete with ATP to bind to the phosphorylation site in the intracellular region of EGFR, inhibit the autophosphorylation process of EGFR and block downstream signaling pathways, thereby achieving the purpose of inhibiting tumor cells. The first-generation reversible EGFR inhibitors, including gefitinib, have a good effect on patients with non-small cell lung cancer, however, acquired drug resistance appears in clinical use. Because the first-generation inhibi...

Claims

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