104479-01-8Relevant articles and documents
Structure-activity relationships of novel anti-malarial agents: Part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides
Wiesner, Jochen,Kettler, Katja,Sakowski, Jacek,Ortmann, Regina,Jomaa, Hassan,Schlitzer, Martin
, p. 361 - 363 (2007/10/03)
We have developed the [5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for anti-malarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The trifluoromethyl substituted derivative displayed an IC50 of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2.
Synthesis, molecular modeling, and structure - Activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors
Sakowski,B?hm,Sattler,Dahse,Schlitzer
, p. 2886 - 2899 (2007/10/03)
Because of the involvement of farnesylated proteins in oncogenesis, inhibition of the protein-modifying enzyme farnesyltransferase is considered a major emerging strategy in cancer therapy. Here, we describe the structure - activity relationship of a nove