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Synthesis of new 1,3-thiazol derivatives of maleopimaric acid as anticancer, antibacterial and antifungal agents.
- Source :
-
Natural product research [Nat Prod Res] 2021 Apr; Vol. 35 (8), pp. 1340-1348. Date of Electronic Publication: 2019 Aug 20. - Publication Year :
- 2021
-
Abstract
- A series of new 1,3-thiazole derivatives of maleopimaric acid 6a-f , 7a-f were synthesized and evaluated for anticancer, antibacterial and antifungal activities. Evaluation of cytotoxic activity against human embryonic kidney 293 cells (HEK293), human neuroblastoma cell line (SH-SY5Y), hepatocellular carcinoma cell line (HepG2) and human T-cell lymphoblast-like line (Jurkat), showed that introduction of the aminothiazole fragment at position 6 of the diterpenoid molecule leads to decrease of cell viability. Substance 3 was found to be the most active against all tested cell lines, inhibiting cell viability with IC <subscript>50</subscript> values in the range of 2-24 μM. The structure-activity relationship of these compounds was studied and the results show that the compounds 6c and 7e exhibited in vitro antifungal activity against Candida albicans and also possessed antibacterial profile against Enterobacter aerogenes , Klebsiella pneumoniae , Staphylococcus aureus , Streptococcus pyogenes , Escherichia coli and Proteus vulgaris .
- Subjects :
- Anti-Bacterial Agents chemistry
Antifungal Agents chemistry
Antineoplastic Agents chemistry
Bacteria drug effects
Candida albicans drug effects
Cell Death drug effects
Cell Line
Humans
Microbial Sensitivity Tests
Structure-Activity Relationship
Thiazoles chemistry
Triterpenes chemistry
Anti-Bacterial Agents pharmacology
Antifungal Agents pharmacology
Antineoplastic Agents pharmacology
Thiazoles chemical synthesis
Thiazoles pharmacology
Triterpenes chemical synthesis
Triterpenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1478-6427
- Volume :
- 35
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Natural product research
- Publication Type :
- Academic Journal
- Accession number :
- 31429302
- Full Text :
- https://doi.org/10.1080/14786419.2019.1648459