51686-52-3Relevant academic research and scientific papers
Synthesis, biological evaluation and mechanism study of a class of benzylideneindanone derivatives as novel anticancer agents
Hu, Jinhui,Yan, Jun,Chen, Jie,Pang, Yanqing,Huang, Ling,Li, Xingshu
, p. 1318 - 1327 (2015/07/15)
A series of new benzylideneindanone derivatives were designed, synthesized and evaluated as antitumor agents. Structure-activity relationship (SAR) studies showed that derivatives with 4,5,6-trimethoxyl on an indanone moiety displayed good anti-proliferative activities. Especially, compound 5a demonstrated the most potent inhibitory activity, with GI50 values from 0.172 to 0.57 μM for five kinds of cancer cell lines. Further investigation showed that 5a could inhibit microtubule polymerization and thus induce G2/M phase arrest and apoptosis in A549 cells. Our findings revealed the benzylideneindanone moiety as a new attractive scaffold for mitosis-targeting drug discovery.
Rational design of novel, potent small molecule pan-selectin antagonists
Kranich, Remo,Busemann, Anke S.,Bock, Daniel,Schroeter-Maas, Sabine,Beyer, Diana,Heinemann, Bo,Meyer, Michael,Schierhorn, Katrin,Zahlten, Rainer,Wolff, Gerhard,Aydt, Ewald M.
, p. 1101 - 1115 (2007/10/03)
This report describes the first results of a rational hit-finding strategy to design novel small molecule antiinflammatory drugs targeting selectins, a family of three cellular adhesion molecules. Based on recent progress in understanding of molecular interaction between selectins and their natural ligands as well as progress in clinical development of synthetic antagonists like 1 (bimosiamose, TBC1269), this study was initiated to discover small molecule selectin antagonists with improved pharmacological properties. Considering 1 as template structure, a ligand-based approach followed by focused chemical synthesis has been applied to yield novel synthetic small molecules (MWr 500) with a trihydroxybenzene motif, bearing neither peptidic nor glycosidic components, with nanomolar in vitro activity. Biological evaluation involves two kinds of in vitro assays, a static molecular binding assay, and a dynamic HL-60 cell attachment assay. As compared to controls, the novel compounds showed improved biological in vitro activity both under static and dynamic conditions.
Combretastatin analogs with tubulin binding activity
-
Page/Page column 30, (2008/06/13)
Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.
Novel conformationally restricted tetracyclic analogs of δ8- tetrahydrocannabinol
Khanolkar, Atmaram D.,Lu, Dai,Fan, Pusheng,Tian, Xiaoyu,Makriyannis, Alexandros
, p. 2119 - 2124 (2007/10/03)
Novel analogs of (-)-Δ8-tetrahydrocannabinol (Δ8-THC) in which the conformation of the side chain was restricted by incorporating the first one or two carbons into a six membered ring fused with the aromatic phenolic A ring were synt
An approach to the biomimetic synthesis of aryltetralin lignans
Pelter, Andrew,Ward, Robert S.,Rao, Ramohan R.
, p. 2933 - 2938 (2007/10/02)
The BF3 catalysed cyclisation of 3-arylpropyl substituted quinone-methide ketals affords a mild, biomimetic route to aryltetralins. 1H- and 13C-NMR spectra of the products are reported.
