Synthesis and Antitumor Activity Evaluation of 2-Aminothiazoles Appended 5-methylisoxazoline and Pyridine-piperazine Hybrid Molecules

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Synthesis and Antitumor Activity Evaluation of 2-Aminothiazoles Appended 5-methylisoxazoline and Pyridine-piperazine Hybrid Molecules

Authors
Type
Published Article
Journal
Letters in Organic Chemistry
Publisher
Bentham Science
Publication Date
Nov 04, 2018
Volume
15
Issue
12
Pages
1070–1077
Identifiers
DOI: 10.2174/1570178615666180430122641
Source
MyScienceWork
License
Green

Abstract

A highly efficient and milder protocol for the syntheses of novel series of 2-aminothiazoles bearing 5-methylisoxazoline and pyridine-piperazine hybrid molecules has been developed. The target compounds 13a-e were screened for their in vitro cytotoxicity activity against various tumor cell lines including MCF-7 (human breast adenocarcinoma), HCT-116 (colorectal carcinoma), Jurkat (human T-cell leukemia) and THP-1 (human acute monocytic leukemia). The bioactive assay showed most of the new compounds exhibited promising results in comparison with the parental Sunitinib. The synthesized compounds could well be used in the future as lead anticancer drugs in drug development studies. The synthesized compounds were fully characterized by IR, 1 H NMR, 13 C NMR, elemental analysis and mass spectral data.

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