159783-25-2Relevant academic research and scientific papers
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer
La Regina, Giuseppe,Bai, Ruoli,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Passacantilli, Sara,Mazzoccoli, Carmela,Ruggieri, Vitalba,Sisinni, Lorenza,Bolognesi, Alessio,Rensen, Whilelmina Maria,Miele, Andrea,Nalli, Marianna,Alfonsi, Romina,Di Marcotullio, Lucia,Gulino, Alberto,Brancale, Andrea,Novellino, Ettore,Dondio, Giulio,Vultaggio, Stefania,Varasi, Mario,Mercurio, Ciro,Hamel, Ernest,Lavia, Patrizia,Silvestri, Romano
, p. 6531 - 6552 (2014/10/16)
We synthesized 3-aroyl-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 3-(3,4,5-trimethoxyphenyl)carbonyl moieties were mandatory to achieve potent inhi
Pharmacological validation of trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness
Bland, Nicholas D.,Wang, Cuihua,Tallman, Craig,Gustafson, Alden E.,Wang, Zhouxi,Ashton, Trent D.,Ochiana, Stefan O.,McAllister, Gregory,Cotter, Kristina,Fang, Anna P.,Gechijian, Lara,Garceau, Norman,Gangurde, Rajiv,Ortenberg, Ron,Ondrechen, Mary Jo,Campbell, Robert K.,Pollastri, Michael P.
experimental part, p. 8188 - 8194 (2012/01/13)
Neglected tropical disease drug discovery requires application of pragmatic and efficient methods for development of new therapeutic agents. In this report, we describe our target repurposing efforts for the essential phosphodiesterase (PDE) enzymes TbrPDEB1 and TbrPDEB2 of Trypanosoma brucei, the causative agent for human African trypanosomiasis (HAT). We describe protein expression and purification, assay development, and benchmark screening of a collection of 20 established human PDE inhibitors. We disclose that the human PDE4 inhibitor piclamilast, and some of its analogues, show modest inhibition of TbrPDEB1 and B2 and quickly kill the bloodstream form of the subspecies T. brucei brucei. We also report the development of a homology model of TbrPDEB1 that is useful for understanding the compound-enzyme interactions and for comparing the parasitic and human enzymes. Our profiling and early medicinal chemistry results strongly suggest that human PDE4 chemotypes represent a better starting point for optimization of TbrPDEB inhibitors than those that target any other human PDEs.
Regioselectivity in direct arylation of benzanilide possessing oxygen substituent in the benzoyl part using palladium without phosphine ligand
Harayama, Takashi,Nagura, Chie,Miyagoe, Taeko,Kawata, Yuko,Abe, Hitoshi,Takeuchi, Yasuo
experimental part, p. 2609 - 2616 (2011/04/15)
The direct arylation of benzanilide (1) possessing ether oxygen(s) in benzoyl part was examined under phosphine ligand-free conditions, which afforded ortho-product (2) and para-product (3) in very similar ratio to presence of P(o-Tol)3 conditi
