1. Biological activity, design, synthesis and structure activity relationship of some novel derivatives of curcumin containing sulfonamides.
- Author
-
Lal J, Gupta SK, Thavaselvam D, and Agarwal DD
- Subjects
- Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemistry, Antifungal Agents chemical synthesis, Antifungal Agents chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Proliferation drug effects, Curcumin chemical synthesis, Curcumin chemistry, Dose-Response Relationship, Drug, Drug Design, Drug Screening Assays, Antitumor, HCT116 Cells, HeLa Cells, Hep G2 Cells, Humans, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship, Sulfonamides chemistry, Anti-Bacterial Agents pharmacology, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Antifungal Agents pharmacology, Antineoplastic Agents pharmacology, Bacteria drug effects, Curcumin pharmacology, Fungi drug effects
- Abstract
Five series of curcumin derivatives with sulfonamides 3a-3e, 4a-4e, 5a-5e, 6a-6e and 7a-7e have been synthesized and evaluated for in vitro antibacterial activity against selected medically important gram-(+) and gram-(-) bacterial species viz. Staphylococcus aureus, Bacillus cereus, Salmonella typhi, Pseudomonas aeruginosa and Escherichia coli, and antifungal activity against few pathogenic fungal species viz. Aspergillus niger, Aspergillus flavus, Trichoderma viride and Curvularia lunata. The cytotoxicity has been determined by measuring IC50 values against human cell lines HeLa, Hep G-2, QG-56 and HCT-116. Among the compounds screened, 3a-3e showed the most potent biological activity against tested bacteria and fungi. Compounds 3a-3e displayed higher cytotoxicity than curcumin. The curcumin derivatives were also evaluated for in vivo anti-inflammatory activity. In contrast, the compounds 6a-6e and 7a-7e showed dramatically decrease in biological activity., (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)
- Published
- 2013
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