- Synthesis and anticancer activity of cyclotriphosphazenes functionalized with 4-methyl-7-hydroxycoumarin
-
As an important branch of heterocyclic compounds, coumarin and its derivatives with diverse potential biological activities have attracted wide attention and have been applied in medical-related fields. In this article, three cyclotriphosphazene derivatives bearing 4-methyl-7-hydroxycoumarin moieties with the numbers of 2, 4, and 6 were synthesized and characterized and their antitumor activities were investigated. All the new compounds were found to display antitumor activity in vitro against breast cancer cell lines (MCF-7 and 4T1 cells) with the IC50 values in the range of 108.72-188.44 μM and 75.93-154.91 μM, respectively. In contrast, the coumarin monomer displayed the values of 4140 μM and 1640 μM (IC50). Our results suggested that the antitumor activity was significantly enhanced when coumarin was introduced onto the surface of cyclotriphosphazenes, thereby providing potent candidate molecules for pharmaceutical applications.
- Chen, Jipeng,Wang, Le,Fan, Yu,Yang, Yunxia,Xu, Mengsheng,Shi, Xiangyang
-
-
Read Online
- Tf2O-Promoted Activating Strategy of Phosphate Analogues: Synthesis of Mixed Phosphates and Phosphinate
-
A metal-, toxic chloride reagent-free activating strategy of various phosphates has been developed. This method enables the facile synthesis of functional phosphates such as alkyl phosphates, aza phosphates, thiophosphate, and mixed diaryl phosphates. A transient phosphorylpyridin-1-ium species in situ generated from phosphates with Tf2O/pyridine readily undergoes a substitution reaction with diverse nucleophiles to form versatile phosphate compounds.
- Huang, Hai,Ash, Jeffrey,Kang, Jun Yong
-
supporting information
p. 4938 - 4941
(2018/08/24)
-
- Synthesis and anticholinesterase activity of some new fluorogenic analogues of organophosphorus nerve agents
-
Eighteen new fluorogenic analogues of organophosphorus nerve agents were synthesised and characterised. They included analogues of tabun, sarin, cyclosarin, soman, VX, and Russian VX, with the 7-oxy-4-methylcoumarin or 7-oxy-4-(trifluoromethyl)coumarin leaving group. These analogues inhibited acetylcholinesterase (AChE) effectively in vitro and therefore have potential as tools for the identification of novel organophosphatases in biological systems. Analogues of VX and Russian VX with the 7-amino-4-methylcoumarin group, although poor AChE inhibitors, may have utility for screening enzyme libraries for phosphoramidases capable of cleaving P-N bonds.
- Timperley, Christopher M.,Casey, Krystal E.,Notman, Stuart,Sellers, David J.,Williams, Nancy E.,Williams, Nichola H.,Williams, Gareth R.
-
p. 1554 - 1563
(2008/09/18)
-
- PHOTOCHEMISTRY OF PESTICIDES, 13. SOME PHOTOREACTIONS OF O,O-DIETHYL-O-(4-METHYL-2-OXO-2H-1-BENZOPYRAN-7-YL)-PHOSPHOROTHIOATE (POTASAN)
-
UV-irradiation (λ>313 nm) of O,O-diethyl-O-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-phosphorothioate (Potasan) 1a in chloroform and/or methanol with and without singlet oxygen results in the formation of the 2-oxo-2H-1-benzopyran-phosphate 2 the 3,3'-bipotasan dehydrodimer 3, and 7-ethoxy-4-methyl-2-oxo-2H-1-benzopyran 4; the mechanisms of formation, especially for 4 are discussed.
- Abdou, Wafaa M.,Mahran, M. Refat,Sidky, Mahmoud M.,Wamhoff, Heinrich
-
p. 199 - 204
(2007/10/02)
-
