Synthesis and docking studies on styryl chromones exhibiting cytotoxicity in human breast cancer cell line.

Abstract

The search for small molecules that preferentially target the functionally important surfaces of estrogen receptor and disrupt the transcriptional activity in the cell has emerged as a promising area towards rationale based drug design. Herein, we report substituted styryl chromones as a new class of compounds that exhibit selectivity for ERbeta binding at the second binding site of HT and antiproliferative activity in human breast cancer cell line.

• Authors: Seema Bhatnagar, Shakti Sahi, Puneet Kackar, Swati Kaushik, Manan K Dave, Akshara Shukla, Ashita Goel
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 16 Pg. 4945-50 (Aug 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20621472 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Benzopyrans
• Chromones
• Estrogen Receptor beta
• Styrenes

Topics

• Antineoplastic Agents (chemical synthesis, therapeutic use, toxicity)
• Benzopyrans (chemical synthesis, pharmacology, therapeutic use)
• Binding Sites
• Breast Neoplasms (drug therapy)
• Cell Line, Tumor
• Chromones (chemistry, therapeutic use, toxicity)
• Computer Simulation
• Drug Design
• Estrogen Receptor beta (chemistry)
• Female
• Humans
• Styrenes (chemical synthesis, pharmacology, therapeutic use)
• Thermodynamics