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Synthesis and cytotoxicity screening of derivatives of the simplified ecteinascidin pentacyclic skeleton as anticancer agents

Guo, Ju ; Yang, Yang ; Wang, Nan ; Liu, Zhanzhu

Tetrahedron Letters, 15 August 2018, Vol.59(33), pp.3202-3205 [Peer Reviewed Journal]

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  • Title:
    Synthesis and cytotoxicity screening of derivatives of the simplified ecteinascidin pentacyclic skeleton as anticancer agents
  • Author: Guo, Ju ; Yang, Yang ; Wang, Nan ; Liu, Zhanzhu
  • Description: A series of new ecteinascidin pentacyclic-derived compounds bearing aryl carboxylic amide side chains at C-22 have been designed and synthesized. The cytotoxicity evaluation confirmed their potent antitumor activity by use of eight different cell lines. Studies on the structure-activity relationship of them showed that the chemical structure of C-22 pendants have great effects on the tumor-killing activity. Notably, Compounds , and with benzo[ ]thiophene-2-carboxamide pendants exhibited excellent broad-spectrum antitumor activity with the low IC values of 10  M.
  • Is Part Of: Tetrahedron Letters, 15 August 2018, Vol.59(33), pp.3202-3205
  • Identifier: ISSN: 0040-4039 ; E-ISSN: 1873-3581 ; DOI: 10.1016/j.tetlet.2018.07.027
  • Subjects: Ecteinascidin Pentacyclic Skeleton ; Synthesis ; Cytotoxicity ; Structure-Activity Relationship ; Chemistry
  • Language: English
  • Source: ScienceDirect Journals (Elsevier)

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