683275-32-3Relevant academic research and scientific papers
Structure - Activity relationships of novel anti-malarial agents. Part 2: Cinnamic acid derivatives
Wiesner, Jochen,Mitsch, Andreas,Wissner, Pia,Jomaa, Hassan,Schlitzer, Martin
, p. 423 - 424 (2001)
We have described compound 1 as a lead structure for a novel class of anti-malarial agents. Replacement of the 3-phenylpropionyl moiety of the lead structure 1 by a 4-propoxycinnamic acid residue resulted in a significant improvement in anti-malarial activity. Compound 3q represents an important step in the development of lead structure 1 into an anti-malarial drug candidate.
Non-thiol farnesyltransferase inhibitors: Utilization of the far aryl binding site by 5-cinnamoylaminobenzophenones
Mitsch, Andreas,Wissner, Pia,Boehm, Markus,Silber, Katrin,Klebe, Gerhard,Sattler, Isabel,Schlitzer, Martin
, p. 493 - 501 (2007/10/03)
We recently described two novel aryl binding sites of farnesyltransferase. In this study, the cinnamoyl residue was designed as an appropriate substituent for our benzophenone-based AAX-peptidomimetic compound capable of occupying the far aryl binding site.
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
