Abstract
3-N-substituted-estrogen derivatives were synthesized and characterized. Their antiproliferative activities against human ER (+) MCF-7 (Breast), ER (-) MDA-MB-231 (breast) and Ishikawa (endometrial) cancer cell lines were determined after 72 hours drug exposure employing CellTiter-Glo assay at concentrations ranging from (0.01-100,000 nM). The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen) and raloxifene (RAL). In vitro results indicated that compound 5 (IC50 = 12µM) displayed comparable antiproliferative activity against MDA-MB 231 cell line; while compounds 6, 7 and 13 (IC50 = 12µM) displayed higher activity against MCF-7 and Ishikawa cell lines, in comparison to TAM activity (19-33µM).
Keywords: 3-N-substituted estrogen derivatives, antiproliferative activity, breast cancer.
Mini-Reviews in Medicinal Chemistry
Title:Synthesis and Biological Activity of 3-N-Substituted Estrogen Derivatives as Breast Cancer Agents
Volume: 13 Issue: 9
Author(s): Zhongliang Wan, Musiliyu A Musa, Patrick Joseph and John S. Cooperwood
Affiliation:
Keywords: 3-N-substituted estrogen derivatives, antiproliferative activity, breast cancer.
Abstract: 3-N-substituted-estrogen derivatives were synthesized and characterized. Their antiproliferative activities against human ER (+) MCF-7 (Breast), ER (-) MDA-MB-231 (breast) and Ishikawa (endometrial) cancer cell lines were determined after 72 hours drug exposure employing CellTiter-Glo assay at concentrations ranging from (0.01-100,000 nM). The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen) and raloxifene (RAL). In vitro results indicated that compound 5 (IC50 = 12µM) displayed comparable antiproliferative activity against MDA-MB 231 cell line; while compounds 6, 7 and 13 (IC50 = 12µM) displayed higher activity against MCF-7 and Ishikawa cell lines, in comparison to TAM activity (19-33µM).
Export Options
About this article
Cite this article as:
Wan Zhongliang, Musa A Musiliyu, Joseph Patrick and Cooperwood S. John, Synthesis and Biological Activity of 3-N-Substituted Estrogen Derivatives as Breast Cancer Agents, Mini-Reviews in Medicinal Chemistry 2013; 13 (9) . https://dx.doi.org/10.2174/1389557511313090012
DOI https://dx.doi.org/10.2174/1389557511313090012 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Aberrant Splicing, Hyaluronan Synthases and Intracellular Hyaluronan as Drivers of Oncogenesis and Potential Drug Targets
Current Cancer Drug Targets GnRH Agonists and Antagonists in Cancer Therapy
Current Medicinal Chemistry - Anti-Cancer Agents MATra - Magnet Assisted Transfection: Combining Nanotechnology and Magnetic Forces to Improve Intracellular Delivery of Nucleic Acids
Current Pharmaceutical Biotechnology Minimally Invasive Approach to Endometrial Cancer: Robotics and Laparoscopy
Current Women`s Health Reviews Network Pharmacology-Based and Molecular Docking Analysis of Resveratrol’s Pharmacological Effects on Type I Endometrial Cancer
Anti-Cancer Agents in Medicinal Chemistry Translating Mismatch Repair Mechanism into Cancer Care
Current Drug Targets Image-Guided Nanoparticle-Based siRNA Delivery for Cancer Therapy
Current Pharmaceutical Design Effects of Estrogens on Atherogenesis
Current Vascular Pharmacology Mechanisms of Drug Resistance in Cancer Chemotherapy: Coordinated Role and Regulation of Efflux Transporters and Metabolizing Enzymes
Current Pharmaceutical Design A Review: The Anti-inflammatory, Anticancer and Antibacterial Properties of Four Kinds of Licorice Flavonoids Isolated from Licorice
Current Medicinal Chemistry Mitochondrial Dysfunction and Targeted Drugs: A Focus on Diabetes
Current Pharmaceutical Design Identification of Disease-Relevant Genes for Molecularly-Targeted Drug Discovery
Current Cancer Drug Targets Drug Targeting of Estrogen Receptor Signaling in the Cardiovascular System: Preclinical and Clinical Studies
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Pleiotropic Effects of Cardioactive Glycosides
Current Medicinal Chemistry Insights into the Role of mTOR/AMPK as a Potential Target for Anticancer Therapy
Current Drug Therapy Imaging Requirements for Personalized Medicine: The Oncologists Point of View
Current Pharmaceutical Design Combination of DC Vaccine and Conventional Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry Flavonoids as Prospective Aromatase Inhibitors in Breast Cancer Prevention/ Therapy
Current Molecular Pharmacology Expression and Prognostic Significance of the MMP Family Molecules in Bladder Cancer
Combinatorial Chemistry & High Throughput Screening Microenvironmental Regulation of Cancer Stem Cell Phenotypes
Current Stem Cell Research & Therapy