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Discovery of N-(Naphtho[1,2-b]Furan-5-Yl) Benzenesulfonamides as Novel Selective Inhibitors of Triple-Negative Breast Cancer (TNBC)
- Source :
- Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry, Molecules; Volume 23; Issue 3; Pages: 678, Molecules, Vol 23, Iss 3, p 678 (2018)
- Publication Year :
- 2018
- Publisher :
- MDPI, 2018.
-
Abstract
- Any type of breast cancer not expressing genes of the estrogen receptor (ER), progesterone receptor (PR), or human epidermal growth factor receptor 2 (HER2) is referred to as triple-negative breast cancer (TNBC). Accordingly, TNBCs do not respond to hormonal therapies or medicines targeting the ER, PR, or HER2. Systemic chemotherapy is therefore the only treatment option available today and prognoses remain poor. We report the discovery and characterization of N-(naphtho[1,2-b]furan-5-yl)benzenesulfonamides as selective inhibitors of TNBCs. These inhibitors were identified by virtual screening and inhibited different TNBC cell lines with IC50 values of 2–3 μM. The compounds did not inhibit normal (i.e. MCF-7 and MCF-10A) cells in vitro, indicating their selectivity against TNBC cells. Considering the selectivity of these inhibitors for TNBC, these compounds and analogs can serve as a promising starting point for further research on effective TNBC inhibitors.
- Subjects :
- 0301 basic medicine
Models, Molecular
Cell Survival
Pharmaceutical Science
Estrogen receptor
Antineoplastic Agents
Triple Negative Breast Neoplasms
Article
Analytical Chemistry
lcsh:QD241-441
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Breast cancer
lcsh:Organic chemistry
three-dimensional similarity search
Furan
Cell Line, Tumor
Drug Discovery
Progesterone receptor
medicine
Humans
Computer Simulation
Physical and Theoretical Chemistry
skin and connective tissue diseases
Furans
Triple-negative breast cancer
Cell Proliferation
Virtual screening
Sulfonamides
Chemistry
Systemic chemotherapy
Organic Chemistry
selective inhibitors
medicine.disease
virtual screening
In vitro
Gene Expression Regulation, Neoplastic
030104 developmental biology
triple-negative breast cancer
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Cancer research
MCF-7 Cells
Molecular Medicine
Female
Drug Screening Assays, Antitumor
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 23
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
- Accession number :
- edsair.doi.dedup.....eb6c4069edd7711b6d6d0054283e9c6c