Bioorganic & medicinal chemistry letters, 2015-07, Vol.25 (13), p.2690-2693
2015
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Details
- Autor(en) / Beteiligte
- Titel
- Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2015-07, Vol.25 (13), p.2690-2693
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2015
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- [Display omitted] In our continuing search for camptothecin (CPT)-derived antitumor drugs, novel structurally diverse PEG-based 20(S)-CPT sulfonylamidine derivatives were designed, synthesized via a Cu-multicomponent reaction (MCR), and evaluated for cytotoxicity against four human tumor cell lines (A-549, MDA-MB-231, KB, and KBvin). All of the derivatives showed promising in vitro cytotoxic activity against the tested tumor cell lines, and were more potent than irinotecan. Significantly, these derivatives exhibited comparable cytotoxicity against KBvin, while irinotecan was less active against this cell line. With a concise efficient synthesis and potent cytotoxic profiles, especially significant activity towards KBvin, these compounds merit further development as a new generation of CPT-derived PEG-conjugated drug candidates.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2015.04.060Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4768722
- Format
- –
- Schlagworte
- Antineoplastic Agents - chemical synthesis, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, C-20 position, Camptothecin, Camptothecin - analogs & derivatives, Camptothecin - chemical synthesis, Camptothecin - chemistry, Camptothecin - pharmacology, Catalysis, Cell Line, Tumor, Cell Proliferation - drug effects, Copper, Cytotoxic activity, Drug Design, Drug Screening Assays, Antitumor, Humans, Irinotecan, KB Cells, Poly(ethylene glycol) (PEG), Polyethylene Glycols - chemical synthesis, Polyethylene Glycols - chemistry, Polyethylene Glycols - pharmacology, Structure-Activity Relationship, Sulfonylamidine