Next Article in Journal
The Effect of an Optimized Wet Milling Technology on the Crystallinity, Morphology and Dissolution Properties of Micro- and Nanonized Meloxicam
Next Article in Special Issue
A Convenient Synthesis of 3,7′-Bisindole Derivatives
Previous Article in Journal
Delivery of Gemcitabine Prodrugs Employing Mesoporous Silica Nanoparticles
Previous Article in Special Issue
A Green Ultrasound Synthesis, Characterization and Antibacterial Evaluation of 1,4-Disubstituted 1,2,3-Triazoles Tethering Bioactive Benzothiazole Nucleus
 
Search for Articles:
Title / Keyword
Author / Affiliation
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
Journals
Molecules
Volume 21
Issue 4
10.3390/molecules21040514
molecules-logo
Submit to this Journal Review for this Journal Edit a Special Issue
► Article Menu

Article Menu

share announcement question_answer thumb_up
...
textsms
...
Article

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

by
Ye-Hui Shi
1,
Dong-Fang Dai
2,3,
Jing Li
2,3,
Yan-Wei Dong
2,3,
Yin Jiang
2,3,
Huan-Gong Li
2,3,
Yuan Gao
2,3,
Chuan-Ke Chong
2,3,
Hui-Ying Li
3,
Xiao-Qian Chu
3,
Cheng Yang
2,3,
Quan Zhang
2,
Zhong-Sheng Tong
1,*,
Cui-Gai Bai
3,* and
Yue Chen
2,*
1
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
2
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
3
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
Molecules 2016, 21(4), 514; https://doi.org/10.3390/molecules21040514
Received: 17 December 2015 / Revised: 8 April 2016 / Accepted: 13 April 2016 / Published: 21 April 2016
(This article belongs to the Collection Heterocyclic Compounds)
View Full-Text Download PDF
Browse Figures

Abstract

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+
►▼ Show Figures

Graphical abstract

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
SciFeed

Share and Cite

MDPI and ACS Style

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. https://doi.org/10.3390/molecules21040514

AMA Style

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(4):514. https://doi.org/10.3390/molecules21040514

Chicago/Turabian Style

Shi, Ye-Hui, Dong-Fang Dai, Jing Li, Yan-Wei Dong, Yin Jiang, Huan-Gong Li, Yuan Gao, Chuan-Ke Chong, Hui-Ying Li, Xiao-Qian Chu, Cheng Yang, Quan Zhang, Zhong-Sheng Tong, Cui-Gai Bai, and Yue Chen. 2016. "Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines" Molecules 21, no. 4: 514. https://doi.org/10.3390/molecules21040514

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Metrics

Article Access Map by Country/Region

1
Back to TopTop