696601-52-2Relevant academic research and scientific papers
Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor
Dalal, Kush,Morin, Helene,Ban, Fuqiang,Shepherd, Ashley,Fernandez, Michael,Tam, Kevin J.,Li, Huifang,LeBlanc, Eric,Lack, Nathan,Prinz, Helge,Rennie, Paul S.,Cherkasov, Artem
, p. 1164 - 1173 (2018/09/12)
The androgen receptor (AR) is a hormone-activated transcription factor that regulates the development and progression of prostate cancer (PCa) and represents one of the most well-established drug targets. Currently clinically approved small molecule inhib
Synthesis, antiprolife ativeactivity and inhibition of tubulinpolymerization by 1,5-and 1,8-disubstituted 10H-anthracen-9-onesbearinga 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety
Nickel, Holger C.,Schmidt, Peter,B?hm, Konrad J.,Baasner, Silke,Müller, Klaus,Gerlach, Matthias,Unger, Eberhard,Günther, Eckhard G.,Prinz, Helge
experimental part, p. 3420 - 3438 (2010/08/20)
A novel series of 1,5-and 1,8-disubstituted 10-benzylidene-10H-anthracen-9- ones and 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones was synthesized to assess the substituent effects on biological activity. The 3-hydroxy-2,4- dimethoxy-benzylidene analogue 16h displayed strong antiproliferative activity against several tumor cell lines,including multi-drug resistant phenotypes. Flow cytometric studies showed that KB/HeLa cells treated by elected compounds were arrested in the G2/M phases of the cell cycle. Among the compounds tested for inhibition of tubulin polymerization,14 compounds proved to be exceptionally active with IC50 values 1 mM. In the 1,5-dichloro-derived series of benzy-lideneanthracenones,E/Z isomers were separated and biological effects were monitored. We found that the olefinic geometry had no significant effect on biological activity. Furthermore,the E isomeric 1,5-dichloro-substituted phenacylidenes entirely proved to be more potent inhibitors of tubulin polymerization than the recently described 10-(2-oxo-2-phenylethylidene)-10H- anthracen-9-ones. In conclusion,the present study improves understanding of the action of anthracenone-based tubulin polymerization inhibitors and contributes to the design of further potent anti-tubulin drugs.
