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Design, synthesis, and anti-proliferative activity of 1-(4-methoxyphenyl)-12-hydroxymethyl-p-carborane derivatives.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2016 Oct 21; Vol. 122, pp. 257-263. Date of Electronic Publication: 2016 Jun 18. - Publication Year :
- 2016
-
Abstract
- 1-(4-Methoxyphenyl)-12-hydroxymethyl-p-carborane (2a), which is a precursor to the previously developed potent carborane-containing ER agonist BE120, exhibited weak cell growth inhibitory activity against four human cancer cell lines (MCF-7, MDA-MB-453, LNCaP, and PC-3). The biological evaluation of a series of derivatives of 2a revealed that an increased number of methoxy groups on the benzene ring of 2a enhanced the cell growth inhibitory activity. Trimethoxyphenyl derivative 2g afforded the most potent cell growth inhibitory activity (mean GI50 value: 5.8 μM) in a panel screening using 39 human cancer cell lines. Moreover, 2g induced for MDA-MB-453 breast cancer cell lines an arrest of the cell cycle in the G2/M phase and apoptosis mediated by caspase-3/7.<br /> (Copyright © 2016 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Antineoplastic Agents metabolism
Apoptosis drug effects
Binding, Competitive
Boranes chemistry
Boranes metabolism
Cell Line, Tumor
Cell Proliferation drug effects
Chemistry Techniques, Synthetic
Drug Screening Assays, Antitumor
Estrogen Receptor alpha metabolism
Humans
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Boranes chemical synthesis
Boranes pharmacology
Drug Design
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 122
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27371927
- Full Text :
- https://doi.org/10.1016/j.ejmech.2016.06.029