Synthesis, Encapsulation and Antitumor Activity of New Betulin Derivatives | Zendy

Csuk René | Zendy; Barthel Alexander | Zendy; Sczepek Ronny | Zendy; Siewert Bianka | Zendy; Schwarz Stefan | Zendy

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Synthesis, Encapsulation and Antitumor Activity of New Betulin Derivatives

Author(s) -

Csuk René,

Barthel Alexander,

Sczepek Ronny,

Siewert Bianka,

Schwarz Stefan

Publication year - 2011

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.201000232

Subject(s) - betulinic acid , betulin , chemistry , cytotoxicity , dna laddering , stereochemistry , apoptosis , combinatorial chemistry , organic chemistry , biochemistry , programmed cell death , dna fragmentation , in vitro , genetics , biology

Novel betulin derivatives were prepared and tested for their antitumor activity. Starting from 3‐ O ‐acetyl‐ or 3‐ O ‐methyl‐betulinic aldehyde, the synthesis of C‐28 ethynyl derivatives was performed; their subsequent transformation with several 1,3‐dipolarophiles afforded pyrazoles and 1,2,3‐triazoles. Their screening for antitumor activity was performed in a panel of 15 human cancer cell lines by a colorimetric SRB‐assay. Thereby, several compounds revealed a higher cytotoxicity than betulinic acid. In addition, the encapsulation of the lead structure 7 into liposomes was investigated. The results from a dye exclusion test and from DNA laddering experiments provided evidence for an apoptotic cell death.

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