Design, synthesis and cytotoxicity of cell death mechanism of rotundic acid derivatives

In the present investigation, 16 new rotundic acid (RA) derivatives modified at the C-3, C-23 and C-28 positions were synthesized. The cytotoxicities of the derivatives were evaluated against HeLa, A375, HepG2, SPC-A1 and NCI-H446 human tumor cell lines by MTT assay. Among these derivatives, compoun...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-05, Vol.23 (9), p.2543-2547
Main Authors: He, Yu-Fang, Nan, Min-Lun, Sun, Jia-Ming, Meng, Zhao-Jie, Li, Wei, Zhang, Ming
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
bcl-2-Associated X Protein - metabolism
Caspase 3 - metabolism
caspase-3
cell growth
Cell Line, Tumor
chemistry
chemotherapy
Cytotoxicity
Derivative
Drug Design
Drug Screening Assays, Antitumor
HeLa Cells
Hep G2 Cells
Humans
inhibitory concentration 50
protein synthesis
Proto-Oncogene Proteins c-bcl-2 - metabolism
Rotundic acid
Triterpenes - chemical synthesis
Triterpenes - chemistry
Triterpenes - pharmacology
Western blotting
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Summary:In the present investigation, 16 new rotundic acid (RA) derivatives modified at the C-3, C-23 and C-28 positions were synthesized. The cytotoxicities of the derivatives were evaluated against HeLa, A375, HepG2, SPC-A1 and NCI-H446 human tumor cell lines by MTT assay. Among these derivatives, compounds 4–7 exhibited stronger cell growth inhibitory than RA and compound 4 was found to be the best inhibition activity on five human tumor cell lines with IC50
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.03.005