Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20
| Autor: | Lasse Evensen, Jürgen Borlak, James B. Lorens, Daniele Passarella, Lisa Dalla Via, Stella Borrelli, Daniela Comi, Bruno Danieli, Ornella Gia, Elena Riva, Gabriele Fontana, Francesco Colombo |
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| Rok vydání: | 2010 |
| Předmět: |
camptothecin derivative
Stereochemistry Clinical Biochemistry Pharmaceutical Science Angiogenesis Inhibitors Antineoplastic Agents inhibition of angiogenesis topoisomerase inhibition Biochemistry Chemical synthesis Inhibitory Concentration 50 Mice Structure-Activity Relationship Cell Line Tumor Drug Discovery medicine Animals Humans Molecular Biology Caspase Cell Proliferation biology Chemistry Cell growth Topoisomerase Organic Chemistry Biological activity DNA Topoisomerases Type I Epidermoid carcinoma Apoptosis Caspases biology.protein Molecular Medicine Camptothecin Topoisomerase I Inhibitors Reactive Oxygen Species medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:8660-8668 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2010.09.069 |
| Popis: | The preparation and biological evaluation of a novel series of dimeric camptothecin derivatives are described. All the new compounds showed a significant ability to inhibit human tumor cell growth with IC50 values ranging from 0.03 to 12.2 μM. The interference with the activity of the nuclear enzymes topoisomerases has been demonstrated, highlighting the poison effect of one of the obtained byproducts toward topoisomerase I. A moderate antiangiogenic activity has been demonstrated for one of the obtained compounds. Moreover, the effects of four new compounds on caspases activity and ROS generation have been studied on transgenic mouse cell. |
| Databáze: | OpenAIRE |
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