Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Presser, A; Lainer, G; Kretschmer, N; Schuehly, W; Saf, R; Kaiser, M; Kalt, MM.
Synthesis of Jacaranone-Derived Nitrogenous Cyclohexadienones and Their Antiproliferative and Antiprotozoal Activities.
Molecules. 2018; 23(11):
Doi: 10.3390/molecules23112902
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- Co-Autor*innen der Med Uni Graz
- Kretschmer Nadine
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- Abstract:
- The cytotoxic and antiprotozoal activities of the phytoquinoide, jacaranone, and related compounds have been an ongoing topic in recent drug discovery. Starting from the natural product-derived cyclohexadienone scaffold, a series of nitrogen-containing derivatives were synthesized and subsequently evaluated for their antiproliferative and antiprotozoal activity. Anticancer potency was analyzed using different types of cancer cell lines: MDA-MB-231 breast cancer, CCRF-CEM leukemia, HCT-116 colon cancer, U251 glioblastoma, and, in addition, non-tumorigenic MRC-5 lung fibroblasts. Antiproliferative activities at micromolar concentrations could be shown. Antiprotozoal activity was assessed against Plasmodium falciparum NF54 and Trypanosoma brucei rhodesiense STIB900. For all compounds, selectivity indices (SI) were calculated based on assessed cytotoxicity towards L6 cells. In addition, the structure-activity-relationships and physicochemical parameters of these compounds are discussed.
- Find related publications in this database (using NLM MeSH Indexing)
- Antineoplastic Agents - chemical synthesis
- Antineoplastic Agents - pharmacology
- Antiprotozoal Agents - chemical synthesis
- Antiprotozoal Agents - chemistry
- Antiprotozoal Agents - pharmacology
- Biological Products - chemistry
- Biological Products - pharmacology
- Cell Line -
- Cell Survival -
- Cyclohexenes - chemical synthesis
- Cyclohexenes - chemistry
- Cyclohexenes - pharmacology
- Humans -
- Molecular Structure -
- Parasitic Sensitivity Tests -
- Phytochemicals - chemistry
- Phytochemicals - pharmacology
- Structure-Activity Relationship -
- Find related publications in this database (Keywords)
- antiproliferative activity
- antiprotozoal activity
- green chemistry
- natural products
- jacaranone