190663-25-3Relevant articles and documents
Triflic anhydride mediated synthesis of 3,4-dihydroquinazolines: A three-component one-pot tandem procedure
Magyar, Christina L.,Wall, Tyler J.,Davies, Steven B.,Campbell, Molly V.,Barna, Haven A.,Smith, Sydney R.,Savich, Christopher J.,Mosey, R. Adam
, p. 7995 - 8000 (2019)
A one-pot three-component tandem reaction involving a key Pictet-Spengler-like annulation step has been developed, providing an efficient method for the synthesis of 3,4-dihydroquinazolines in moderate to good yields from amides, aldehydes, and amines. The multicomponent triflic anhydride mediated reaction tolerates the installation of numerous functional groups, affording extensive diversity about the heterocyclic scaffold.
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer
La Regina, Giuseppe,Bai, Ruoli,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Passacantilli, Sara,Mazzoccoli, Carmela,Ruggieri, Vitalba,Verrico, Annalisa,Miele, Andrea,Monti, Ludovica,Nalli, Marianna,Alfonsi, Romina,Di Marcotullio, Lucia,Gulino, Alberto,Ricci, Biancamaria,Soriani, Alessandra,Santoni, Angela,Caraglia, Michele,Porto, Stefania,Da Pozzo, Eleonora,Martini, Claudia,Brancale, Andrea,Marinelli, Luciana,Novellino, Ettore,Vultaggio, Stefania,Varasi, Mario,Mercurio, Ciro,Bigogno, Chiara,Dondio, Giulio,Hamel, Ernest,Lavia, Patrizia,Silvestri, Romano
, p. 5789 - 5807 (2015/08/24)
We designed 39 new 2-phenylindole derivatives as potential anticancer agents bearing the 3,4,5-trimethoxyphenyl moiety with a sulfur, ketone, or methylene bridging group at position 3 of the indole and with halogen or methoxy substituent(s) at positions 4-7. Compounds 33 and 44 strongly inhibited the growth of the P-glycoprotein-overexpressing multi-drug-resistant cell lines NCI/ADR-RES and Messa/Dx5. At 10 nM, 33 and 44 stimulated the cytotoxic activity of NK cells. At 20-50 nM, 33 and 44 arrested >80% of HeLa cells in the G2/M phase of the cell cycle, with stable arrest of mitotic progression. Cell cycle arrest was followed by cell death. Indoles 33, 44, and 81 showed strong inhibition of the SAG-induced Hedgehog signaling activation in NIH3T3 Shh-Light II cells with IC50 values of 19, 72, and 38 nM, respectively. Compounds of this class potently inhibited tubulin polymerization and cancer cell growth, including stimulation of natural killer cell cytotoxic activity and repression of Hedgehog-dependent cancer.
1-(2-alkanamidoethyl)-6-methoxyindole derivatives: A new class of potent indole melatonin analogues
Tarzia, Giorgio,Diamantini, Giuseppe,Di Giacomo, Barbara,Spadoni, Gilberto,Esposti, Daniele,Nonno, Romolo,Lucini, Valeria,Pannacci, Marilou,Fraschini, Franco,Stankov, Bojidar Michaylov
, p. 2003 - 2010 (2007/10/03)
A new series of indole melatonin analogues, bearing the amido ethyl side chain attached at the N-1 position of the indole nucleus, were synthesized and tested for their affinity for the melatonin receptor isolated from quail optic tecta in a series of in
