- One-pot synthesis of highly functionalized benzo [1,3] thiazine from isocyanides, aniline, and heterocumulene via Cu-catalyzed intramolecular C-H activation reactions
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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
- Dastjerdi, Hossein F.,Nematpour, Manijeh,Rezaee, Elham,Jahani, Mehdi,Tabatabai, Sayyed A.
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p. 1537 - 1541
(2019/07/12)
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- Cobalt mediated by desulfurization toward the synthesis of isothiocyanates
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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.
- Seelam, Mohan,Shaik, Bajivali,Kammela, Prasada Rao
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supporting information
p. 1759 - 1765
(2016/10/31)
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- Design, synthesis and biological evaluation of thiourea and nicotinamide-containing sorafenib analogs as antitumor agents
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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.
- Kong, Xiangkai,Yao, Zeyu,He, Zuopeng,Xu, Wenfang,Yao, Jianwen
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supporting information
p. 867 - 870
(2015/05/27)
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- Design, synthesis and antiproliferative activities of diaryl thiourea derivatives as anticancer agents
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Two new series of diaryl thiourea containing sorafenib derivatives 9a-9t were designed and synthesized, and their antiproliferative activities against PC-3, HCT116 and MDA-MB-231 cell lines were evaluated. All compounds generally showed antiproliferative activity to PC-3 cells, most of the analogs exhibited potent antiproliferative activity to HCT116 cells, and compounds 9e, 9f, 9o and 9p demonstrated inhibitory activities against all three cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS. Two series of diaryl thiourea derivatives have been designed, prepared, and tested for cytotoxicity against human tumor cells PC-3, HCT116 and MDA-MB-231. The results showed that all compounds generally had antiproliferative activity against PC-3 cells, and some compounds demonstrated competitive antiproliferative activities to sorafenib. Copyright
- Yao, Jianwen,He, Zuopeng,Chen, Jing,Chen, Daquan,Sun, Wei,Xu, Wenfang
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p. 2423 - 2430,8
(2020/09/16)
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- Microwave-assisted synthesis and antibacterial activity of novel chenodeoxycholic acid thiosemicarbazone derivatives
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A rapid and efficient method for the synthesis of novel chenodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave irradiation is reported. Ten novel compounds have been synthesised in good yields. Their structures were elucidated by 1H NMR, IR, ESI-MS spectra and elemental analysis. Preliminary results showed that some of these compounds possess inhibitory effects against S. typhimurium and E. coli.
- Qiu, Liying,Shi, Zhichuan,Mei, Qinggang,Zhao, Zhigang
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experimental part
p. 456 - 459
(2011/11/06)
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- Synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave
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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.
- Shi, Zhi Chuan,Zhao, Zhi Gang,Liu, Xing Li,Chen, Yu
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experimental part
p. 405 - 408
(2012/01/05)
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- Solvent-free synthesis of indole-based thiosemicarbazones under microwave irradiation
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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.
- Liu, Lingling,Yang, Jie,Zhao, Zhigang,Shi, Peiyu,Liu, Xingli
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experimental part
p. 57 - 60
(2010/05/19)
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- Synthesis of novel alkoxycarbonyl thiosemicarbazide molecular tweezers derived from deoxycholic acid under microwave irradiation
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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.
- Chen, Yu,Zhao, Zhi Gang,Liu, Xing Li,Shi, Zhi Chuan
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scheme or table
p. 416 - 420
(2010/12/19)
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- Microwave-assisted synthesis of new steroidal thiosemicarbazones derived from methyl 3-oxocholanate under solvent-free conditions
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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.
- Zhao, Zhigang,Liu, Xingli,Liu, Lingling,Li, Guohua
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experimental part
p. 455 - 458
(2010/12/24)
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