Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors
Guoqiang Dong
1
,
Yuxin Fang
1
,
Y Liu
2
,
Na Liu
1
,
Shanchao Wu
1
,
Wannian Zhang
1
,
Chun-Quan Sheng
1
2
Department of Pharmacy, No. 401 Hospital of Chinese People's Liberation Army, Qingdao 266071, People's Republic of China.
|
Тип публикации: Journal Article
Дата публикации: 2017-05-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
28351590
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
Previously, 4-tosylanthra[1,2-c][1,2,5]thiadiazole-6,11-dione (1) was identified as a novel non-camptothecin topoisomerase I (Top1) inhibitor by structure-based virtual screening. Herein, a series of 4-substituted derivatives were designed and synthesized. Most of them showed potent Top1 inhibitory activity. Their in vitro antiproliferative activity was also evaluated in A549, HCT-116 and ZR-75-30 human cancer cell lines. Compound 8s showed good antiproliferative activity with IC50 of 0.52μM and 0.42μM against HCT-116 and ZR-75-30 cell line, respectively. Top1 unwinding assay and molecular modeling studies rationalized the mode of action of this new class of inhibitors.
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Dong G. et al. Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 9. pp. 1929-1933.
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Dong G., Fang Y., Liu Y., Liu N., Wu S., Zhang W., Sheng C. Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 9. pp. 1929-1933.
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TY - JOUR
DO - 10.1016/j.bmcl.2017.03.039
UR - https://doi.org/10.1016/j.bmcl.2017.03.039
TI - Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Dong, Guoqiang
AU - Fang, Yuxin
AU - Liu, Y
AU - Liu, Na
AU - Wu, Shanchao
AU - Zhang, Wannian
AU - Sheng, Chun-Quan
PY - 2017
DA - 2017/05/01
PB - Elsevier
SP - 1929-1933
IS - 9
VL - 27
PMID - 28351590
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2017_Dong,
author = {Guoqiang Dong and Yuxin Fang and Y Liu and Na Liu and Shanchao Wu and Wannian Zhang and Chun-Quan Sheng},
title = {Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2017},
volume = {27},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/j.bmcl.2017.03.039},
number = {9},
pages = {1929--1933},
doi = {10.1016/j.bmcl.2017.03.039}
}
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MLA
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Dong, Guoqiang, et al. “Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 27, no. 9, May. 2017, pp. 1929-1933. https://doi.org/10.1016/j.bmcl.2017.03.039.