397330-61-9Relevant articles and documents
Synthesis and biological evaluation of novel Jiyuan Oridonin A-1,2,3-triazole-azole derivatives as antiproliferative agents
Ke, Yu,Liang, Jian-Jia,Hou, Rui-Juan,Li, Ming-Ming,Zhao, Long-Fei,Wang, Wang,Liu, Ying,Xie, Hang,Yang, Rui-Hua,Hu, Tian-Xing,Wang, Jin-Yi,Liu, Hong-Min
, p. 1249 - 1263 (2018)
As a continuation of our research on developing potent and potentially safe anti-proliferative agents, two series of novel Jiyuan Oridonin A-1,2,3-triazole-azole hybrids were designed, synthesized and evaluated for their anti-proliferative activity against four selected cancer cell lines (MGC-803, MCF-7, PC-3, Eca-109). Some compounds with better growth inhibitory effects were chosen to carry out further studies in A549 and SMMC-7721. Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Particularly, the most active agent 8b showed high potency against human cancer cells with IC50 ranging from 0.2 ± 0.0 to 5.0 ± 0.9 μM. Cellular mechanism studies elucidated compound 8b arrests cell cycle at G1 phase and induce a strong apoptotic response in SMMC-7721 cells. Furthermore, 8b could inhibit the colony formation and migration via Wnt signaling pathway in SMMC-7721 cells. For all these reasons, compound 8b holds promising potential as anti-proliferative agent.
A library of spirooxindoles based on a stereoselective three-component coupling reaction
Lo, Michael M.-C.,Neumann, Christopher S.,Nagayama, Satoshi,Perlstein, Ethan O.,Schreiber, Stuart L.
, p. 16077 - 16086 (2007/10/03)
A collection of structurally complex and chemically diverse small molecules is a useful tool to explore cell circuitry. In this article, we report the split-pool synthesis of more than 3000 spirooxindoles on high capacity macrobeads. The key reaction to a
Synthesis and cytotoxicity of 3-(hetarylthio)-1-propynyl-(trimethyl)silanes
Abele,Abele,Rubina,Dzenitis,Arsenyan,Shestakova,Nesterova,Domracheva,Popelis,Grinberga,Lukevics
, p. 867 - 872 (2007/10/03)
We have developed a two-step method for synthesis of 3-(hetarylthio)-1-propynyl(trimethyl)silanes from thiols in a phase-transfer catalysis system HC≡CCH2Br-solid K2CO3-18-crown-6-toluene followed by reaction with n-BuLi-Me3SiCl in ether or THF. We have observed that 3-[1,3-bis(trimethylsilyl)-2-propynyl] thioindole displays high cytotoxicity in HT-1080 and MG-22A tumor cell lines.