4548-56-5Relevant articles and documents
BTB-1 A small molecule inhibitor of the mitotic motor protein kif18A
Catarinella, Mario,Gruener, Tamara,Strittmatter, Tobias,Marx, Andreas,Mayer, Thomas U.
, p. 9072 - 9076 (2009)
Turning the motor off: A malachite green based assay leads to the identification of BTB-1 (see picture), the first small-molecule inhibitor of the mitotic motor protein Kif18A. BTB-1 reversibly inhibits the ATPase activity of the recombinant motor domain
Quinazolinone and isoquinolinone derivative
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Paragraph 0319; 0320, (2016/10/08)
The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors
García, Ana M.,Brea, José,Morales-García, Jose A.,Perez, Daniel I.,González, Alejandro,Alonso-Gil, Sandra,Gracia-Rubio, Irene,Ros-Simó, Clara,Conde, Santiago,Cadavid, María Isabel,Loza, María Isabel,Perez-Castillo, Ana,Valverde, Olga,Martinez, Ana,Gil, Carmen
, p. 8590 - 8607 (2014/12/11)
A forward chemical genetic approach was followed to discover new targets and lead compounds for Parkinson's disease (PD) treatment. By analysis of the cell protection produced by some small molecules, a diphenyl sulfide compound was revealed to be a new phosphodiesterase 7 (PDE7) inhibitor and identified as a new hit. This result allows us to confirm the utility of PDE7 inhibitors as a potential pharmacological treatment of PD. On the basis of these data, a diverse family of diphenyl sulfides has been developed and pharmacologically evaluated in the present work. Moreover, to gain insight into the safety of PDE7 inhibitors for human chronic treatment, we evaluated the new compounds in a surrogate emesis model, showing nonemetic effects.