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Synthesis and Research of 2-aminthiazole Compouds as PTKs Inhibitors

Author: YeWei
Tutor: YuYongPing
School: Zhejiang University
Course: Medicinal Chemistry
Keywords: Compound libraries Tyrosine kinase inhibitors Activity Zhejiang University Inhibitory activity Chronic myeloid leukemia QSAR Small molecules Protein tyrosine kinases Amino
CLC: R914
Type: Master's thesis
Year: 2010
Downloads: 191
Quote: 0
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Abstract


The research of anticancer drugs has always been an important task in the R&D of new drugs. During the past few years, the role of protein tyrosine kinases(PTKs) palying in the malignant proliferation of tumour cell has been studied and revealed, and consequently the PTKs has been an important target to find a new drug. Many effective drugs of PTKs inhibitor have appeared on market while much more kinds of PTKs inhibitor molecule are in the clinical trial. 2-aminthiazole has been proved novel Src family kinase inhibitor template and Dasatinib(BMS-354825 ) has been on sale as a significant Bcr-Able kinase inhibitor to treat Chronic Myeloid Leukemia(CML). So 2-aminthiazole compounds have great value in anticancer drugs research.A new library of 2-aminthiazole-5-carboxylates was built, which would be screened in biochemical and cellular assays, in order to find a new high potent PTKs inhibitor. 6 kinds of amins and 40 kinds of carboxylic acids or isocyanates were bound to the template, so that a convenient rout was designed to build the library. About 116 compounds have been synthesised in this way, which are all new. On the basis of the cell-inhebition experiment, the QSAR of these compounds can be studied.45 compounds have been chosen to detect the inhebition activity to K562 cell strain, with the purpose to find good compouds to treat CML desease. 25 of the compouds can inhebit the regular growth of the tumor cell. A preliminary discussion of the QSAR have been given at the last part of this article.

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CLC: > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry
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