852990-39-7Relevant articles and documents
Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization
Hong, Yilang,Zhao, Yinglin,Yang, Lei,Gao, Minghuan,Li, Long,Man, Shuai,Wang, Zhan,Guan, Qi,Bao, Kai,Zuo, Daiying,Wu, Yingliang,Zhang, Weige
, p. 287 - 296 (2019/06/14)
Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n′ and 7n′′ showed remarkable antiproliferative activities agai
Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4
Guan, Qi,Yang, Fushan,Guo, Dandan,Xu, Jingwen,Jiang, Mingyang,Liu, Chunjiang,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 1 - 9 (2015/02/05)
A set of novel selenium-containing heterocyclic analogues of combretastatin A-4 (CA-4) have been designed and synthesised using a rigid 1,2,5-selenadiazole as a linker to fix the cis-orientation of ring-A and ring-B. All of the target compounds were evalu
Synthesis and antitumor activity of benzils related to combretastatin A-4
Mousset, Celine,Giraud, Anne,Provot, Olivier,Hamze, Abdallah,Bignon, Jerome,Liu, Jian-Miao,Thoret, Sylviane,Dubois, Joelle,Brion, Jean-Daniel,Alami, Mouad
scheme or table, p. 3266 - 3271 (2009/04/05)
A series of benzil derivatives related to combretastatin A-4 (CA-4) have been synthesized by oxidation of diarylalkynes promoted by PdI2 in DMSO. Using this new protocol, 14 benzils were prepared in good to excellent yields and their biological
Microwave-assisted efficient synthesis of 1,2-diaryldiketones: a novel oxidation reaction of diarylalkynes with DMSO promoted by FeBr3
Giraud, Anne,Provot, Olivier,Peyrat, Jean-Fran?ois,Alami, Mouad,Brion, Jean-Daniel
, p. 7667 - 7673 (2007/10/03)
This paper reports the oxidation of functionalized diarylalkynes with DMSO in the presence of the environmentally friendly FeBr3 catalyst. This non-toxic procedure is general and has been applied successfully under microwave irradiation leading rapidly to benzil derivatives in good yields.
Synthesis and cytotoxic evaluation of combretafurazans
Tron, Gian Cesare,Pagliai, Francesca,Del Grosso, Erika,Genazzani, Armando A.,Sorba, Giovanni
, p. 3260 - 3268 (2007/10/03)
Combretastatin A-4 is an antitumoral and antitubulin agent that is active only in its cis configuration. In the present manuscript, we have synthesized cis-locked combretastatins embodying a furazan ring (combretafurazans). To achieve this, we have developed a new strategy that exploits the dehydration of vicinal dioximes using the Mitsunobu reaction. Among the advantages of following such a strategy are the mild conditions used for the construction of the diarylfurazan derivatives, allowing for the presence of highly functionalized substrates and deactivated aromatic rings. Combretafurazans are more potent in vitro cytotoxic compounds compared to combretastatins in neuroblastoma cells, yet maintaining similar structure-activity relationship and pharmacodynamic profiles.