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Issue 71, 2018
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Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer

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Abstract

Arsenic trioxide (As2O3) has been approved for the treatment of acute promyelocytic leukemia (APL); however, its use in the treatment of solid tumors is limited due to its pharmacokinetic properties. Organic arsenic compounds provide better options for pharmaceutical optimization. p-Aminophenyl arsenoxide (p-APAO), an organic arsenic compound, was found to interact with the promyelocytic leukemia–retinoic acid receptor alpha (PML–RARα) fusion protein in a similar manner to arsenic trioxide. Analogs of p-APAO such as 4-(1,3,2-dithiarsolan-2-yl)aniline (p-APDTAs) were recently found to show improved cytotoxicity toward several solid tumor cell lines with lower toxicity to normal cells. Here, we synthesized a carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline (p-APDTAs) and showed that it exhibited reduced cytotoxicity to normal cells, suggesting a feasible approach to improve the therapeutic index of arsenic-containing compounds as chemotherapeutic agents.

Graphical abstract: Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer

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Publication details

The article was received on 21 Sep 2018, accepted on 24 Nov 2018 and first published on 05 Dec 2018


Article type: Paper
DOI: 10.1039/C8RA07860B
RSC Adv., 2018,8, 40760-40764
  • Open access: Creative Commons BY-NC license
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    Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer

    B. Fu, X. Wang, Y. Li, J. Hu, D. Lu, W. Li, K. Zheng and C. Qin, RSC Adv., 2018, 8, 40760
    DOI: 10.1039/C8RA07860B

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