Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents
Yu-Ru Lee
1, 2
,
Tsung-Wen Chen
3
,
Chia Chung Lee
3
,
Chun-Liang Chen
3
,
Ahmed Atef Ahmed Ali
1, 4
,
Jih-Hwa Guh
6
,
Dah-Shyong Yu
2
,
Hsu-Shan Huang
1, 7
Publication type: Journal Article
Publication date: 2015-09-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
26344783
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
A series of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-diones were synthesized and evaluated using the cell proliferations, apoptosis and NCI-60 cell panel assays. Also, the signaling pathways that account for their activities were investigated. Compounds 2, 3, 4a, 4d, 4f, 4i, 4k, 5b, 5c, 5d, 5f, 5g, 6b, 6c, 6d, 6e, 6g, 7a and 7g were selected by NCI. Among the tested compounds, 6g appeared to be the most active compound of this series that not only induced apoptosis in DU-145 cancer cells but also attenuated the ERK1/2 and p38 signaling pathways. All test compounds exhibited diverse cytostatic and cytotoxic activities that warrant further development as potential anticancer agents.
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28
Total citations:
28
Citations from 2024:
6
(21.42%)
Cite this
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GOST
Copy
Lee Y. et al. Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents // European Journal of Medicinal Chemistry. 2015. Vol. 102. pp. 661-676.
GOST all authors (up to 50)
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Lee Y., Chen T., Lee C. C., Chen C., Ali A. A. A., Tikhomirov A. S., Guh J., Yu D., Huang H. Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents // European Journal of Medicinal Chemistry. 2015. Vol. 102. pp. 661-676.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.ejmech.2015.07.052
UR - https://doi.org/10.1016/j.ejmech.2015.07.052
TI - Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents
T2 - European Journal of Medicinal Chemistry
AU - Lee, Yu-Ru
AU - Chen, Tsung-Wen
AU - Lee, Chia Chung
AU - Chen, Chun-Liang
AU - Ali, Ahmed Atef Ahmed
AU - Tikhomirov, Alexander S
AU - Guh, Jih-Hwa
AU - Yu, Dah-Shyong
AU - Huang, Hsu-Shan
PY - 2015
DA - 2015/09/01
PB - Elsevier
SP - 661-676
VL - 102
PMID - 26344783
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2015_Lee,
author = {Yu-Ru Lee and Tsung-Wen Chen and Chia Chung Lee and Chun-Liang Chen and Ahmed Atef Ahmed Ali and Alexander S Tikhomirov and Jih-Hwa Guh and Dah-Shyong Yu and Hsu-Shan Huang},
title = {Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents},
journal = {European Journal of Medicinal Chemistry},
year = {2015},
volume = {102},
publisher = {Elsevier},
month = {sep},
url = {https://doi.org/10.1016/j.ejmech.2015.07.052},
pages = {661--676},
doi = {10.1016/j.ejmech.2015.07.052}
}
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