Journal
CHEMISTRYSELECT
Volume 4, Issue 2, Pages 742-746Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201803664
Keywords
2,4 '-linked oligothiazole; 2-phenylthiazole; thiasporine A; anithiactins A-C; antitumor activity
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Funding
- National Natural Science Foundation of China [21402192, 21507040]
- Key Laboratory of Marine Ecology and Environment Science and Engineering, SOA [MESE-2017-06]
- Natural Science Foundation of Shandong Province [ZR2017-QD008]
- State Key Laboratory of Environmental Chemistry and Ecotoxicology [KF2015-07]
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Directly 2,4-linked oligothiazoles are not only broadly applied in drug discovery but also are the core structural motif of many biological natural products. With this background, we reported a simple and efficient route for the synthesis of four 2-phenylthiazole natural products anithiactins A-C, thiasporine A, and series of their novel 2,4-linked oligothiazole derivatives relies on the one-pot cascade reaction of beta-azido disulfides and commercially carboxyl acids. This approach also represented a remarkably direct and simple route for 2,4-linked oligothiazoles synthesis. By doing so, ten bisthiazoles and terthiazoles were effectively obtained in only 3 similar to 6 linear steps with good to moderate yields. The bioassay results demonstrated that all the phenyl-based oligothiazoles show potent antitumor activities. Among them, terthiazole 28 was the most potent compound with IC50 values of 4.4 mu M, 4.8 mu M against HCT116 and A549 cell lines, respectively.
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