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Synthesis and Cytotoxicity of N-Substituted Dibenzo[a,j]xanthene-3,11-dicarboxamide Derivatives.

ABSTRACT: In order to study the structure-activity relationships of xanthene derivatives, four series of N-substituted 14-aryl-14H-dibenzo[a,j]xanthene-3,11-dicarboxamide derivatives were synthesized. The structures of all compounds were identified by ¹H-NMR, HR-MS and IR spectra, in which compounds 6a-h were further identified by ¹³C-NMR spectra. The in vitro antitumor activity of the synthesized compounds was tested by MTT assay. Most of them displayed strong inhibitory activity on human hepatocellular carcinoma cell lines (SK-HEP-1, HepG2 and SMMC-7721 cells) and acute promyelocytic leukemia NB4 cells. Compounds 6c-6e exhibited significant inhibitory activity against NB4 cells with IC₅₀ values of 0.52 ?M and 0.76 ?M, respectively, much lower than 5.31 ?M of the positive control As?O?.

SUBMITTER: Song Y

PROVIDER: S-EPMC6154592 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Synthesis and Cytotoxicity of N-Substituted Dibenzo[a,j]xanthene-3,11-dicarboxamide Derivatives.

Song Yongbin Y Yang Yihui Y Wu Lijun L Dong Naiwei N Gao Shang S Ji Hongrui H Du Xia X Liu Bo B Chen Guoyou G

Molecules (Basel, Switzerland) 20170323 4

In order to study the structure-activity relationships of xanthene derivatives, four series of N-substituted 14-aryl-14H-dibenzo[a,j]xanthene-3,11-dicarboxamide derivatives were synthesized. The structures of all compounds were identified by ¹H-NMR, HR-MS and IR spectra, in which compounds 6a-h were further identified by 13C-NMR spectra. The in vitro antitumor activity of the synthesized compounds was tested by MTT assay. Most of them displayed strong inhib ...[more]

PMID: 28333112

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