15867-09-1Relevant articles and documents
One-pot synthesis of highly functionalized benzo [1,3] thiazine from isocyanides, aniline, and heterocumulene via Cu-catalyzed intramolecular C-H activation reactions
Dastjerdi, Hossein F.,Nematpour, Manijeh,Rezaee, Elham,Jahani, Mehdi,Tabatabai, Sayyed A.
, p. 1537 - 1541 (2019/07/12)
A one-pot synthesis of functionalized benzo thiazine derivatives via a Cu-catalyzed, multicomponent reaction of isocyanides, aniline, and heterocumulenes in acetonitrile at room temperature was developed. Transition metal-catalyzed activation of C-H bonds
Design, synthesis and biological evaluation of thiourea and nicotinamide-containing sorafenib analogs as antitumor agents
Kong, Xiangkai,Yao, Zeyu,He, Zuopeng,Xu, Wenfang,Yao, Jianwen
supporting information, p. 867 - 870 (2015/05/27)
A series of thiourea and nicotinamide-containing sorafenib analogs (7a-n) were designed and synthesized and their antiproliferative activities were tested against HCT116, MDA-MB-231, PC-3 and HepG2 cell lines. Most of the compounds showed potent activities against the four cell lines, compound 7h showed better activities than sorafenib against all four cell lines, and compounds 7a and 7e showed better activities against HCT116 and MDA-MB-231 cell lines. The anti-angiogenic activities of 7e and 7h were also better than that of sorafenib in both in vitro HUVEC tube formation assay and ex vivo rat thoracic aorta ring assay.
Design, synthesis and biological activities of sorafenib derivatives as antitumor agents
Yao, Jianwen,He, Zuopeng,Chen, Jing,Sun, Wei,Fang, Hao,Xu, Wenfang
, p. 6549 - 6553,5 (2012/12/12)
A series of novel sorafenib derivatives, 9a-w, was designed and synthesized in high yields using various substituted anilines, and their antiproliferative activities against HCT116, PC-3 and MDA-MB-231 cell lines were also evaluated and described. All compounds exhibited potent antiproliferative activity against HCT116 and PC-3 cells with IC50 = 2.8-52.0 and 2.2-45.6 μM; compounds 9p and 9q demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines, the cytotoxicity of compound 9r is more potent than that of sorafenib. Compounds (9g, 9p, 9q and 9r) were chosen for further evaluation of the anti-angiogenesis activity, and showed the inhibition of sprout formation from aortic ring ex vivo. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.
