Synthesis of farnesyl diphosphate analogues containing ether-linked photoactive benzophenones and their application in studies of protein prenyltransferases.

Protein prenylation is a posttranslational lipid modification in which C(15) and C(20) isoprenoid units are linked to specific protein-derived cysteine residues through a thioether linkage. This process is catalyzed by a class of enzymes called prenyltransferases that are being intensively studied due to the finding that Ras protein is farnesylated coupled with the observation that mutant forms of Ras are implicated in a variety of human cancers. Inhibition of this posttranslational modification may serve as a possible cancer chemotherapy.

[Anatomic-therapeutic-chemical classification of drugs].

European Research Association for Pharmaceutical Market and an international group have developed the ADC Drug Classification system, which is recommended by the World Health Organization (WHO). It has been in use since 1987. According to this classification, drugs are grouped into fourteen basic groups according to the organic system of the organism where they work.

Photoactive Analogs of Farnesyl Pyrophosphate Containing Benzoylbenzoate Esters: Synthesis and Application to Photoaffinity Labeling of Yeast Protein Farnesyltransferase.

Farnesyl pyrophosphate (FPP) is involved in a large number of cellular processes including the prenylation of transforming mutants of Ras proteins implicated in cancer. Photoactive analogs could provide useful information about enzyme active sites that bind farnesyl pyrophosphate; however, the availability of such compounds is extremely limited. Molecules that incorporate benzophenone moieties are attractive photoaffinity labeling reagents because of their useful photochemical properties.

Reactivity and microbiological activity of 2-methyl-3-carboethoxy-5-pyrrolinone derivatives.

This work describes the synthesis of 2-methyl-3-carboethoxy-5-pyrrolinone which was then allowed to react with aromatic aldehydes, nitromethines, benzendiazonium salts, hydrazine and amines. Several of the products have shown good results in preliminary antimicrobial and antifungal tests.

Synthesis and antimicrobiological activity of N-aryl-substituted 2-methyl-3-carbethoxy-5-pyrrolinone derivatives.

We describe the synthesis of N-aryl-2-methyl-3-carbethoxy-5-pyrrolinones benzylidene derivatives, their condensation with azomethines and substitution with aniline. The compounds have been tested for antimicrobial and fungicide activity: they have better fungicidal than bactericidal activity.