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

[ Vol. 15 , Issue. 12 ]

Author(s):

Garbapu Suresh*, Ratnakaram Venkata Nadh, Navuluri Srinivasu and Durgaprasad Yennity   Pages 1070 - 1077 ( 8 )

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.

Affiliation:

Division of Chemistry, Department of Science and Humanities, Vignan's Foundation for Science Technology and Research University, Guntur-522213, GITAM University - Bengaluru Campus, Karnataka - 561203, Division of Chemistry, Department of Science and Humanities, Vignan's Foundation for Science Technology and Research University, Guntur-522213, Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr.HomiBhabha Road, Pune-411008

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