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

Author(s): Garbapu Suresh*, Ratnakaram Venkata Nadh, Navuluri Srinivasu, Durgaprasad Yennity.

Journal Name: Letters in Organic Chemistry

Volume 15 , Issue 12 , 2018

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Graphical 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 that the 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, 1H NMR, 13C NMR, elemental analysis and mass spectral data.

Keywords: Hybrid drugs, antiproliferative activity, 2-aminothiazole, pyridine-piperazine scaffold, 5-methylisoxazoline, anticancer drug.

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Article Details

Year: 2018
Page: [1070 - 1077]
Pages: 8
DOI: 10.2174/1570178615666180430122641
Price: $65

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