5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells
Mingying Wang
1
,
Baojia Sun
2
,
Ye Tao
1
,
Yanbing Wang
3
,
Yonglian Hou
1
,
Siyuan Wang
4
,
Huaqi Pan
5
,
Huiming Hua
1
,
Dahong Li
1
2
Yantai Valiant Pharmaceutical Co. Ltd., 60, Taiyuan Road, Dajijia Industrial Park, YEDA Yantai, Shandong 264006, PR China
|
Publication type: Journal Article
Publication date: 2023-07-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
37329677
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
27 novel 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A were designed and synthesized to make them more conducive to the cancer treatment. The antiproliferative activity of all the target compounds was tested against six human cancer cell lines and one human normal cell line. Compound 10d exhibited nearly the most potent cytotoxicity with IC50 values of 0.58, 0.69, 1.82, 0.85, 0.75, 0.33 and 1.75 μM against A549, DU-145, A375, HeLa, HepG2, MDA-MB-231 and L-02 cell lines. Moreover, 10d inhibited metastasis and induced apoptosis of MDA-MB-231 cells in a dose-dependent manner. The potent anticancer effects of 10d were prompted based on the aforementioned results, the therapeutic potential of 10d for breast cancer was worth further exploration.
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Wang M. et al. 5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells // Bioorganic and Medicinal Chemistry. 2023. Vol. 90. p. 117380.
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Wang M., Sun B., Tao Y., Wang Y., Hou Y., Wang S., Pan H., Hua H., Li D. 5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells // Bioorganic and Medicinal Chemistry. 2023. Vol. 90. p. 117380.
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TY - JOUR
DO - 10.1016/j.bmc.2023.117380
UR - https://doi.org/10.1016/j.bmc.2023.117380
TI - 5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells
T2 - Bioorganic and Medicinal Chemistry
AU - Wang, Mingying
AU - Sun, Baojia
AU - Tao, Ye
AU - Wang, Yanbing
AU - Hou, Yonglian
AU - Wang, Siyuan
AU - Pan, Huaqi
AU - Hua, Huiming
AU - Li, Dahong
PY - 2023
DA - 2023/07/01
PB - Elsevier
SP - 117380
VL - 90
PMID - 37329677
SN - 0968-0896
SN - 1464-3391
ER -
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BibTex (up to 50 authors)
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@article{2023_Wang,
author = {Mingying Wang and Baojia Sun and Ye Tao and Yanbing Wang and Yonglian Hou and Siyuan Wang and Huaqi Pan and Huiming Hua and Dahong Li},
title = {5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells},
journal = {Bioorganic and Medicinal Chemistry},
year = {2023},
volume = {90},
publisher = {Elsevier},
month = {jul},
url = {https://doi.org/10.1016/j.bmc.2023.117380},
pages = {117380},
doi = {10.1016/j.bmc.2023.117380}
}