Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

Celastrol is a natural triterpenoid which possesses diverse pharmacological activities including potent antitumor activity. Previously, we reported a C(6)-modified celastrol derivative NST001A which possesses cytotoxic activity against Colon 205 cells with a 60 nM IC 50 value. To further explore the...

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Bibliographic Details
Published inRSC advances Vol. 5; no. 25; pp. 19620 - 19623
Main Authors Tang, Kaiyong, Huang, Jinwen, Pan, Junfang, Zhang, Xuan, Lu, Wei
Format Journal Article
LanguageEnglish
Published 01.01.2015
Subjects
Anticancer properties
Biological
Biotechnology
Cancer
Colon
Derivatives
Human
Synthesis
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Summary:Celastrol is a natural triterpenoid which possesses diverse pharmacological activities including potent antitumor activity. Previously, we reported a C(6)-modified celastrol derivative NST001A which possesses cytotoxic activity against Colon 205 cells with a 60 nM IC 50 value. To further explore the structure activity relationships, a new class of C(6)-indole substituted celastrol derivatives were designed and synthesized. Biological evaluation of these compounds includes their cytotoxic activity against human hepatocellular carcinoma Bel7402 and human glioblastoma cell line H4. Among all these semisynthetic analogues, compound 4f and 4h displayed excellent in vitro antiproliferative activities against Bel7402 cancer cells (IC 50 = 0.02 μM and 0.01 μM, respectively).
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ISSN:2046-2069
2046-2069
DOI:10.1039/C4RA15414B