Synthesis, Cytotoxicity and Antimicrobial Evaluation of New Coumarin-Tagged β-Lactam Triazole Hybrid
| Autor: | Prishani Kisten, Paul Awolade, Nosipho Cele, Sanjeev Dhawan, SouravTaru Saha, Mandeep Kaur, Ashona‐Singh Pillay, Parvesh Singh, Sreekantha B. Jonnalagadda |
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| Rok vydání: | 2019 |
| Předmět: |
Antifungal Agents
Triazole Estrogen receptor Bioengineering Antineoplastic Agents Microbial Sensitivity Tests beta-Lactams 01 natural sciences Biochemistry chemistry.chemical_compound Structure-Activity Relationship Coumarins Candida albicans Cytotoxic T cell Humans Cytotoxicity Molecular Biology Cell Proliferation biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Biological activity General Chemistry General Medicine Triazoles biology.organism_classification Antimicrobial Molecular biology 0104 chemical sciences Anti-Bacterial Agents 010404 medicinal & biomolecular chemistry HEK293 Cells chemistry Cell culture Pseudomonas aeruginosa MCF-7 Cells Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Chemistrybiodiversity. 17(1) |
| ISSN: | 1612-1880 |
| Popis: | A series of coumarin-tagged β-lactam triazole hybrids (10a-10o) were synthesized and tested for their cytotoxic activity against MDA-MB-231 (triple negative breast cancer), MCF-7 (estrogen receptor positive breast cancer (ER+)) and A549 (human lung carcinoma) cancer cell lines including one normal cell line, HEK-293 (human embryonic kidney). Two compounds 10b and 10d exhibited substantial cytotoxic effect against MCF-7 cancer cell lines with IC50 values of 53.55 and 58.62 μm, respectively. More importantly, compounds 10b and 10d were non-cytotoxic against HEK-293 cell lines. Structure-activity relationship (SAR) studies suggested that the nitro and chloro group at the C-3 position of phenyl ring are favorable for anticancer activity, particularly against MCF-7 cell lines. Furthermore, antimicrobial evaluation of these compounds revealed modest inhibition of examined pathogenic strains with compounds 10c and 10i being the most promising antimicrobial agents against Pseudomonas aeruginosa and Candida albicans, respectively. |
| Databáze: | OpenAIRE |
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