313499-48-8Relevant academic research and scientific papers
Palladium-catalyzed tandem intramolecular oxy/amino-palladation/isocyanide insertion: Synthesis of α-benzofuranyl/indolylacetamides
Thirupathi, Nuligonda,Hari Babu, Madala,Dwivedi, Vikas,Kant, Ruchir,Sridhar Reddy, Maddi
supporting information, p. 2908 - 2911 (2014/06/23)
A novel palladium-catalyzed approach to 2-benzofuranyl/indolylacetamides from 1-(o-hydroxy/aminophenyl)propargylic alcohols and isocyanides is described. The reaction proceeds through a cascade that includes oxy/aminopalladation, isocyanide insertion, and 1,4-hydroxyl migration. No oxidant or ligand is needed to promote the cascade, and the reactions are carried out under mild conditions to afford the products through high functional tolerance.
Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3- benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity
Kettler, Katja,Wiesner, Jochen,Silber, Katrin,Haebel, Peter,Ortmann, Regina,Sattler, Isabel,Dahse, Hans-Martin,Jomaa, Hassan,Klebe, Gerhard,Schlitzer, Martin
, p. 93 - 101 (2007/10/03)
Water solubility was previously found to be essential for in vivo-antimalarial activity of a novel type of benzophenone-based farnesyltransferase inhibitors. Introduction of a α-amino group into the phenylacetic acid substructure provided more soluble compounds with high farnesyltransferase inhibitory activity. The in vitro-antimalarial activity was detrimentally influenced by this structural modification.
Structure-activity relationships of novel anti-malarial agents. Part 6: N-(4-arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides
Wiesner, Jochen,Fucik, Katharina,Kettler, Katja,Sakowski, Jacek,Ortmann, Regina,Jomaa, Hassan,Schlitzer, Martin
, p. 1539 - 1541 (2007/10/03)
We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into th
Non-thiol farnesyltransferase inhibitors: N-(4-Acylamino-3-benzoylphenyl)-4-nitrocinnamic acid amides
Sakowski, Jacek,Sattler, Isabel,Schlitzer, Martin
, p. 233 - 239 (2007/10/03)
We have developed a 4-nitrocinnamoyl substituted benzophenone as a novel non-thiol farnesyltransferase inhibitor. Replacement of the p-tolyl moiety of our initial lead structure by different para and ortho substituted phenyl residues as well as by 1-naphthyl resulted in derivatives with considerably enhanced activity displaying IC50 values between 42 and 52 nM. These compounds represent novel, readily accessible non-thiol farnesyltransferase inhibitors being more active than the corresponding thiol-containing analogues. Copyright
Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-Acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides
Wiesner, Jochen,Kettler, Katja,Jomaa, Hassan,Schlitzer, Martin
, p. 543 - 545 (2007/10/03)
We have described 5-(4-propoxycinnamoylamino)-2-(4-tolylacetylamino)benzophenone 6e as a novel lead for anti-malarial agents. Anti-malarial activity of these 5-(4-propoxycinnamoylamino)benzophenones proved to be quite sensitive against variations of the a
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
