Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer. Academic Article uri icon

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-RAR) 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.

published proceedings

  • RSC Adv

author list (cited authors)

  • Fu, B., Wang, X., Li, Y., Hu, J., Lu, D., Li, W., Zheng, K., & Qin, C.

citation count

  • 2

complete list of authors

  • Fu, Boqiao||Wang, Xiaolin||Li, Yingjie||Hu, Jingying||Lu, Dai||Li, Wei||Zheng, Kewang||Qin, Caiqin

publication date

  • January 1998