TY - JOUR
T1 - 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
AU - Lee, Yu Ru
AU - Chen, Tsung Chih
AU - Lee, Chia Chung
AU - Chen, Chun Liang
AU - Ahmed Ali, Ahmed Atef
AU - Tikhomirov, Alexander
AU - Guh, Jih Hwa
AU - Yu, Dah Shyong
AU - Huang, Hsu Shan
N1 - Funding Information:
The authors thank the NCI Developmental Therapeutics Program (DTP) for 60 cancer cell line screen of selected compounds described in this paper funded by National Cancer Institute , National Institutes of Health (NIH-NCI). The present study was support by Ministry of Science and Technology and Taipei Medical University grants ( NSC101-2113-M-016 , MOST103-2113-M-038-002 , TMU102-AE1-B32 and TMUTOP-103003-1 to H.S. Huang and NSC102-2314-B-016-048-MY2 to D.S. Yu).
PY - 2015/9/18
Y1 - 2015/9/18
N2 - 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.
AB - 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.
KW - Anthra[1 2-c][1 2 5]thiadiazole-6 11-dione
KW - Apoptosis
KW - NCI 60-cell panel assay
KW - SRB assay
KW - Thiadiazoles
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U2 - 10.1016/j.ejmech.2015.07.052
DO - 10.1016/j.ejmech.2015.07.052
M3 - Article
C2 - 26344783
AN - SCOPUS:84941197893
SN - 0223-5234
VL - 102
SP - 661
EP - 676
JO - CHIM.THER.
JF - CHIM.THER.
ER -
