97026-72-7Relevant academic research and scientific papers
Design, synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybrids
Shi, Wei,Hu, Jinglin,Bao, Na,Li, Dongang,Chen, Li,Sun, Jianbo
supporting information, p. 147 - 151 (2016/12/27)
12 novel scopoletin-isoxazole and scopoletin-pyrazole hybrids were designed, synthesized and their chemical structures were confirmed by HR-MS, IR,1H NMR and13C NMR spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including HCT-116, Hun7 and SW620 by MTT assay. The screening results showed that six compounds (9a, 9c, 9d, 12a, 18b and 18d) exhibited potent cytotoxic activities with IC50values below 20?μM. Besides, we have further evaluated the growth inhibitory activities of six compounds against the human normal tissue cell lines HFL-1. Especially, compound 9d displayed significant anti-proliferative activity with IC50values ranging from 8.76?μM to 9.83?μM and weak cytotoxicity with IC50value of 90.9?μM on normal cells HFL-1, which suggested that isoxazole-based hybrids of scopoletin were an effective chemical modification to improve the anticancer activity of scopoletin.
Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists
Zhang, Xuqing,Cai, Chaozhong,Winters, Michael,Wells, Michele,Wall, Mark,Lanter, James,Sui, Zhihua,Ma, Jingyuan,Novack, Aaron,Nashashibi, Imad,Wang, Yuanping,Yan, Wen,Suckow, Arthur,Hua, Hong,Bell, Austin,Haug, Peter,Clapper, Wilma,Jenkinson, Celia,Gunnet, Joseph,Leonard, James,Murray, William V.
, p. 3272 - 3278 (2017/07/07)
A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
A Thermal Wolf Rearrangement-Benzannulation Route to Naphthisoxazoles, Benzofuro- or isoxazoles and 1,2-Benzisoxazoles
Chen, Ya Ping,Chantegrel, Bernard,Deshayes, Christian
, p. 175 - 186 (2007/10/02)
The title compounds substituted in position 4 by a dimethylphosphono group and in position 5 by a hydroxy group were prepared by the thermal decomposition of dimethyl 2-(5-aryl-(or furyl or alkenyl)-3-methylisoxazol-4-yl)-2-oxo-1-diazoethylphosphonates th
