Diversity oriented synthesis of chromene-xanthene hybrids as anti-breast cancer agents.

Abstract

A diverse library of chromene-xanthene hybrids were synthesized through intramolecular Friedel-Crafts reaction of the arenoxy carbinols. Examples include first incorporation of amino acid tyrosine into xanthene skeletons with polar functionalities. A careful structural evaluation revealed that tyrosine crafted chromene-xanthene hybrids exhibited good activities against breast cancer cell lines MCF-7, MDA-MB-231. The lead compound 16 displays significant cell cycle arrest at G1 phase and induces apoptosis in MDA-MB-231 cells.

• Authors: M Srinivas Lavanya Kumar, Jyotsana Singh, Sudipta Kumar Manna, Saroj Maji, Rituraj Konwar, Gautam Panda
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 28 Issue 4 Pg. 778-782 (02 15 2018) ISSN: 1464-3405 [Electronic] England
• PMID: 29352645 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2018 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Benzopyrans
• Xanthenes
• Tamoxifen

Topics

• Antineoplastic Agents (chemical synthesis, pharmacology, toxicity)
• Apoptosis (drug effects)
• Benzopyrans (chemical synthesis, pharmacology, toxicity)
• Breast Neoplasms (drug therapy)
• Cell Line, Tumor
• G1 Phase Cell Cycle Checkpoints (drug effects)
• HEK293 Cells
• Humans
• Molecular Structure
• Tamoxifen (pharmacology)
• Xanthenes (chemical synthesis, pharmacology, toxicity)