357436-81-8Relevant articles and documents
Benzophenone-based farnesyltransferase inhibitors with high activity against Trypanosoma cruzi
Esteva, Monica I.,Kettler, Katja,Maidana, Cristina,Fichera, Laura,Ruiz, Andrés M.,Bontempi, Esteban J.,Andersson, Bj?rn,Dahse, Hans-Martin,Haebel, Peter,Ortmann, Regina,Klebe, Gerhard,Schlitzer, Martin
, p. 7186 - 7191 (2005)
Less toxic drugs are needed to combat the human parasite Trypanosoma cruzi (Chagas's disease). One novel target for antitrypanosomal drug design is farnesyltransferase. Several farnesyltransferase inhibitors based on the benzophenone scaffold were assayed
Antimalarial and antitrypanosomal activity of a series of amide and sulfonamide derivatives of a 2,5-diaminobenzophenone
Altenkaemper, Mirko,Bechem, Benjamin,Perruchon, Johann,Heinrich, Swetlana,Maedel, Andrea,Ortmann, Regina,Dahse, Hans-Martin,Freunscht, Ellen,Wang, Yulin,Rath, Jennifer,Stich, August,Hitzler, Manuela,Chiba, Peter,Lanzer, Michael,Schlitzer, Martin
experimental part, p. 7690 - 7697 (2010/03/24)
Here, we describe a series of readily obtainable benzophenone derivatives with antimalarial and antitrypanosomal activity. The most active compounds display submicromolar activity against Plasmodium falciparum. Micromolar activity is obtained against Trypanosoma brucei. Main problem of the compounds is low selectivity. However, there are indications that separation of antimalarial and cytotoxic activity might by possible. In addition, some compounds inhibit human ABC transporter with nanomolar activity.
Farnesyltransferase Inhibitors Inhibit the Growth of Malaria Parasites In Vitro and In Vivo
Wiesner, Jochen,Kettler, Katja,Sakowski, Jacek,Ortmann, Regina,Katzin, Alejandro M.,Kimura, Emilia A.,Silber, Katrin,Klebe, Gerhard,Jomaa, Hassan,Schlitzer, Martin
, p. 251 - 254 (2007/10/03)
The inhibition of farnesyltransferase was recently suggested as a new strategy for malaria therapy. A class of farnesyltransferase inhibitors such as 1 has been prepared which have in vivo activity in a murine malaria model. These inhibitors significantly