5410-78-6Relevant articles and documents
Thiourea-containing arsenic sugar with anti-tumor activity and preparation method and application thereof
-
Paragraph 0024; 0026; 0030-0033; 0045-0048, (2020/04/02)
The invention relates to the field of arsenic sugar, and in particular relates to thiourea-containing arsenic sugar with anti-tumor activity and a preparation method and application thereof. The thiourea-containing arsenic sugar is composed of two compounds: 1-(N-(4'-(1'', 3'', 2''-dithiaarsenic pentane-2-yl) phenyl)-thiourea)-2, 3, 4, 6-O-acetyl-beta-D-glucose and 1-(N-(4'-(1'', 3 '', 2''-dithiaarsenic hexane-2-yl) phenyl)-thiourea)-2, 3, 4, 6-O-acetyl-beta-D-glucose. The thiourea-containing arsenic sugar provided by the invention has the advantages of simple reaction operation and high yield. The thiourea-containing arsenic sugar with a specific three-dimensional configuration can be obtained, and the thiourea-containing arsenic sugar has good anti-tumor activity.
Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer
Fu, Boqiao,Wang, Xiaolin,Li, Yingjie,Hu, Jingying,Lu, Dai,Li, Wei,Zheng, Kewang,Qin, Caiqin
, p. 40760 - 40764 (2019/01/03)
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.
Synthesis of a novel C3-symmetric arsine and its application in stereoselective cyclopropanation of electron-deficient olefins
Wang, Changqing
supporting information, p. 7003 - 7005 (2013/01/15)
A novel C3-symmetric arsine was synthesized from p-arsanilic acid in three steps. It was employed in the one-pot cyclopropanation of olefins with carbonyl-stabilized arsonium ylides formed in situ from methyl bromoacetate in the presence of NaH