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Molecules 2016, 21(4), 514; doi:10.3390/molecules21040514

Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines

Department of Breast Oncology, Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer, Key Laboratory of Breast Cancer Prevention and Therapy, Tianjin Medical University, Ministry of Education, and Key Laboratory of Cancer Prevention and Therapy, Tianjin 30060, China
The State Key Laboratory of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, China
High-throughput Molecular Drug Discovery Center, Tianjin International Joint Academy of BioMedicine, Tianjin 300457, China
Authors to whom correspondence should be addressed.
Academic Editor: Richard A. Bunce
Received: 17 December 2015 / Revised: 8 April 2016 / Accepted: 13 April 2016 / Published: 21 April 2016
(This article belongs to the Collection Heterocyclic Compounds)
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Recent studies have shown that sulforaphane (SFN) selectively inhibits the growth of ALDH+ breast cancer stem-like cells.Herein, a series of SFN analogues were synthesized and evaluated against breast cancer cell lines MCF-7 and SUM-159, and the leukemia stem cell-like cell line KG-1a. These SFN analogues were characterized by the replacement of the methyl group with heterocyclic moieties, and the replacement of the sulfoxide group with sulfide or sulfone. A growth inhibitory assay indicated that the tetrazole analogs 3d, 8d and 9d were significantly more potent than SFN against the three cancer cell lines. Compound 14c, the water soluble derivative of tetrazole sulfide 3d, demonstrated higher potency against KG-1a cell line than 3d. SFN, 3d and 14c significantly induced the activation of caspase-3, and reduced the ALDH+ subpopulation in the SUM159 cell line, while the marketed drug doxrubicin(DOX) increased the ALDH+ subpopulation. View Full-Text
Keywords: sulforaphane (SFN); analogues; water soluble derivative; KG-1a; SUM-159; MCF-7; caspase-3; ALDH+ sulforaphane (SFN); analogues; water soluble derivative; KG-1a; SUM-159; MCF-7; caspase-3; ALDH+

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Shi, Y.-H.; Dai, D.-F.; Li, J.; Dong, Y.-W.; Jiang, Y.; Li, H.-G.; Gao, Y.; Chong, C.-K.; Li, H.-Y.; Chu, X.-Q.; Yang, C.; Zhang, Q.; Tong, Z.-S.; Bai, C.-G.; Chen, Y. Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines. Molecules 2016, 21, 514.

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