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Synthesis and anticancer activity of Indolin-2-one derivatives bearing the 4-thiazolidinone moiety.

Abstract
A novel series of indolin-2-one derivatives containing the 4-thiazolidinone moiety (5a-5p) was synthesized and the cytotoxicity of these derivatives was evaluated in vitro against three human cancer cell lines (HT-29, H460 and MDA-MB-231) by standard MTT assay. Some prepared compounds exhibited significant cytotoxicity against different human cancer cell lines. Several potent compounds were further evaluated against one normal cell line (WI-38). In particular, the promising compound 5h showed remarkable cytotoxicity and selectivity against the HT-29 and H460 cancer cell lines (IC(50)  = 0.016 µmol/L, 0.0037 µmol/L, respectively).
AuthorsShuobing Wang, Yanfang Zhao, Wufu Zhu, Ying Liu, Kaixing Guo, Ping Gong
JournalArchiv der Pharmazie (Arch Pharm (Weinheim)) Vol. 345 Issue 1 Pg. 73-80 (Jan 2012) ISSN: 1521-4184 [Electronic] Germany
PMID21932254 (Publication Type: Journal Article)
CopyrightCopyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Chemical References
  • Antineoplastic Agents
  • Indoles
  • Thiazoles
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Culture Techniques
  • Cell Survival (drug effects)
  • Chemistry Techniques, Synthetic
  • Drug Design
  • HT29 Cells
  • Humans
  • Indoles (chemical synthesis, chemistry, pharmacology)
  • Inhibitory Concentration 50
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thiazoles (chemistry)

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