Design, synthesis, anti-proliferative evaluation and docking studies of 1H-1,2,3-triazole tethered ospemifene–isatin conjugates as selective estrogen receptor modulators

2018 ◽  
Vol 42 (5) ◽  
pp. 3703-3713 ◽  
Author(s):  
Sumit Kumar ◽  
Liang Gu ◽  
Gabriella Palma ◽  
Mandeep Kaur ◽  
Ashona Singh-Pillay ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Cell Lines ◽  
Selective Estrogen Receptor Modulators ◽  
Docking Studies ◽  
Design Synthesis ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators ◽  
Mcf 7

A library of 1H-1,2,3-triazole-tethered ospemifene–isatin and ospemifene–spiroisatin conjugates have been synthesized and evaluated for their anti-proliferative activities against MCF-7 and MDA-MB-231 cell lines.

Flexible Estrogen Receptor Modulators:  Design, Synthesis, and Antagonistic Effects in Human MCF-7 Breast Cancer Cells

2001 ◽  
Vol 44 (7) ◽  
pp. 1072-1084 ◽  
Author(s):  
Mary J. Meegan ◽  
Rosario B. Hughes ◽  
David G. Lloyd ◽  
D. Clive Williams ◽  
Daniela M. Zisterer
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Design Synthesis ◽  
Antagonistic Effects ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators ◽  
Mcf 7

scholarly journals A Novel Role for Raloxifene Nanomicelles in Management of Castrate Resistant Prostate Cancer

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Sebastien Taurin ◽  
Hayley Nehoff ◽  
Thalita van Aswegen ◽  
Rhonda J. Rosengren ◽  
Khaled Greish
Keyword(s):  
Prostate Cancer ◽  
Estrogen Receptor ◽  
Cell Lines ◽  
Selective Estrogen Receptor Modulators ◽  
Migration And Invasion ◽  
Prostate Cell ◽  
Estrogen Receptor Modulators ◽  
Castrate Resistant Prostate Cancer ◽  
Castrate Resistant ◽  
Receptor Modulators

Of patients with castrate resistant prostate cancer (CRPC), less than 25–33% survive more than five years. Recent studies have implicated estrogen, acting either alone or synergistically with androgens in the development of castrate resistant prostate cancer. Severalin vitroandin vivostudies, as well as a limited number of clinical trials, have highlighted the potential of selective estrogen receptor modulators, such as raloxifene (Ral) for the treatment of castrate resistant prostate cancer. However, the poor oral bioavailability and metabolism of selective estrogen receptor modulators limit their efficiency in clinical application. To overcome these limitations, we have used styrene co-maleic acid (SMA) micelle to encapsulate raloxifene. Compared to free drug, SMA-Ral micelles had 132 and 140% higher cytotoxicity against PC3 and DU 145 prostate cell lines, respectively. SMA-Ral effectively inhibits cell cycle progression, increases apoptosis, and alters the integrity of tumor spheroid models. In addition, the micellar system induced changes in expression and localization of estrogen receptors, epidermal growth factor receptor (EGFR), and downstream effectors associated with cell proliferation and survival. Finally, SMA-Ral treatment decreased migration and invasion of castrate resistant prostate cancer cell lines. In conclusion, SMA-Ral micelles can potentially benefit new strategies for clinical management of castrate resistant prostate cancer.

ChemInform Abstract: Flexible Estrogen Receptor Modulators: Design, Synthesis, and Antagonistic Effects in Human MCF-7 Breast Cancer Cells.

ChemInform ◽  
2010 ◽  
Vol 32 (27) ◽  
pp. no-no
Author(s):  
Mary J. Meegan ◽  
Rosario B. Hughes ◽  
David G. Lloyd ◽  
D. Clive Williams ◽  
Daniela M. Zisterer
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Design Synthesis ◽  
Antagonistic Effects ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators ◽  
Mcf 7

ChemInform Abstract: Design, Synthesis and Bioevaluation of Novel Candidate Selective Estrogen Receptor Modulators.

ChemInform ◽  
2011 ◽  
Vol 43 (4) ◽  
pp. no-no
Author(s):  
Yogesh Yadav ◽  
Erin D. MacLean ◽  
Annyt Bhattacharyya ◽  
Virinder S. Parmar ◽  
Jan Balzarini ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulators ◽  
Design Synthesis ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators
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