Abstract
Daurinol, a natural aryl naphthalene lactone, has been reported to have antiproliferative activity against various cell lines, and has also been shown to be efficacious in an in vivo xenograft mouse model. In this study, we tried to discover a new scaffold that enables both rapid structure–activity relationship study of daurinol and scalable synthesis of active compounds. 4-Aza-daurinol, a bioisosterism-based scaffold of daurinol, was designed and 17 analogues were synthesized and evaluated against five representative cancer cell lines. Among them, the 2,3-dihydrobenzo[b][1,4]dioxinyl derivative was found to be the most potent and showed similar activity and tendency as daurinol.
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Acknowledgments
This work was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (NRF-2012R1A1A1007057).
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Faisal Hayat and Seung-Hyuk Park have contributed equally to this study.
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Hayat, F., Park, SH., Choi, NS. et al. Synthesis and anticancer activity of 4-aza-daurinol derivatives. Arch. Pharm. Res. 38, 1975–1982 (2015). https://doi.org/10.1007/s12272-015-0619-2
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DOI: https://doi.org/10.1007/s12272-015-0619-2