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
Cobalt mediated by desulfurization toward the synthesis of isothiocyanates
Seelam, Mohan,Shaik, Bajivali,Kammela, Prasada Rao
supporting information, p. 1759 - 1765 (2016/10/31)
A highly efficient and simple protocol for the construction of aromatic and aliphatic isothiocyanates from their respective amines in the presence of cheap, readily available, and air-stable cobalt catalyst is described. All reactions were carried out under optimized reaction conditions and gave target products in good to excellent yields within shorter reaction time.
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.
Thiourea and thioether derivatives of sorafenib: Synthesis, crystal structure, and antiproliferative activity
Yao, Jianwen,Chen, Jing,He, Zuopeng,Sun, Wei,Fang, Hao,Xu, Wenfang
, p. 3959 - 3968 (2013/07/26)
A series of novel sorafenib derivatives containing diaryl thiourea and thioether, 9a-u, was designed and synthesized, and their antiproliferative activities against HCT116 and MDA-MB-231 cell lines were also evaluated and described. Most compounds exhibited potent antiproliferative activity against HCT116 cells with IC50 = 1.8-80.4 μM. Compounds 9p, 9r, and 9s demonstrated competitive antiproliferative activities to sorafenib, against all two cancer cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR, and HRMS, and compound 9n was characterized by single-crystal X-ray diffraction. Primary structure-activity relationships (SAR) have also been established.
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.
Synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave
Shi, Zhi Chuan,Zhao, Zhi Gang,Liu, Xing Li,Chen, Yu
experimental part, p. 405 - 408 (2012/01/05)
An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed. Its main advantages are short reaction times, good conversions and the environmentally friendly nature of the process. The preliminary results indicate that some of these compounds possess inhibitory effects against E. coli.
Solvent-free synthesis of indole-based thiosemicarbazones under microwave irradiation
Liu, Lingling,Yang, Jie,Zhao, Zhigang,Shi, Peiyu,Liu, Xingli
experimental part, p. 57 - 60 (2010/05/19)
A rapid, effi cient and environmentally friendly methodology has been developed for the synthesis of indole-3-carboxaldehyde thiosemicarbazones by using aluminum oxide as the solid support under microwave assisted solvent-free conditions. Compared with the conventional heating method, this method gave the target products in good yield.
Synthesis of novel alkoxycarbonyl thiosemicarbazide molecular tweezers derived from deoxycholic acid under microwave irradiation
Chen, Yu,Zhao, Zhi Gang,Liu, Xing Li,Shi, Zhi Chuan
scheme or table, p. 416 - 420 (2010/12/19)
A series of novel 12α-alkoxycarbonyl thiosemicarbazide molecular tweezers based on 3α-(1-naphthoyl) deoxycholic acid methyl ester were synthesised under microwave irradiation. Their structures were characterised by 1H NMR, IR, MS spectra and elemental analysis. Their chiral recognition properties for the methyl esters of amino acids were investigated. The preliminary results showed that these molecular tweezers have good enantioselective recognition for D/L-amino acid methyl esters.
Microwave-assisted synthesis of new steroidal thiosemicarbazones derived from methyl 3-oxocholanate under solvent-free conditions
Zhao, Zhigang,Liu, Xingli,Liu, Lingling,Li, Guohua
experimental part, p. 455 - 458 (2010/12/24)
A series of novel steroidal thiosemicarbazones derived from methyl 3-oxocholanate were synthesised in good yields via microwave irradiation under solvent-free conditions. The structures of the compounds were confirmed by spectroscopic data. Compared to the conventional method, microwave irradiation was a fast and simple method. These compounds were tested for antibacterial activity against S. aureus, S. pyogenes, and E. coli bacteria.
