Synthesis and antiproliferative activity of benzofuran-based analogs of cercosporamide against non-small cell lung cancer cell lines.

Abstract

A novel series of 3-methyl-1-benzofuran derivatives were synthesized and screened in vitro for their antiproliferative activity against two human NSCLC cell lines (NSCLC-N6 mutant p53 and A549 wild type p53). Most promising compounds presented a structural analogy with the west part of cercosporamide, a natural product of biological interest. In particular, compounds 10, 12 and 31 showed cytotoxic activities at micromolar concentrations (IC₅₀ < 9.3 μM) and compounds 13, 18 and 32 displayed moderate IC₅₀ values (25-40 μM).

• Authors: Marc-Antoine Bazin, Lizeth Bodero, Christophe Tomasoni, Bénédicte Rousseau, Christos Roussakis, Pascal Marchand
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 69 Pg. 823-32 (Nov 2013) ISSN: 1768-3254 [Electronic] France
• PMID: 24121233 (Publication Type: Journal Article)
• Copyright: Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antineoplastic Agents
• Benzofurans
• cercosporamide
• benzofuran

Topics

• Antineoplastic Agents (administration & dosage, chemical synthesis, chemistry, pharmacology)
• Benzofurans (chemical synthesis, chemistry, pharmacology)
• Carcinoma, Non-Small-Cell Lung (drug therapy, pathology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Humans
• Lung Neoplasms (drug therapy, pathology)
• Molecular Structure
• Structure-Activity Relationship