BIOMAT Database Logo BIOMAT Database Logo

Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3-benzoylphenyl)-3-arylfurylacrylic acid amides. 2004

Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, D-35032 Marburg, Germany.

We have designed arylfurylacryl-substituted benzophenones as non-thiol farnesyltransferase inhibitors utilizing a novel aryl binding site of farnesyltransferase. These compounds display activity in the low nanomolar range.

UI MeSH Term Description Entries
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D000179 Acrylates Derivatives of acrylic acid (the structural formula CH2
D000577 Amides Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed) Amide
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D012441 Saccharomyces cerevisiae A species of the genus SACCHAROMYCES, family Saccharomycetaceae, order Saccharomycetales, known as "baker's" or "brewer's" yeast. The dried form is used as a dietary supplement. Baker's Yeast,Brewer's Yeast,Candida robusta,S. cerevisiae,Saccharomyces capensis,Saccharomyces italicus,Saccharomyces oviformis,Saccharomyces uvarum var. melibiosus,Yeast, Baker's,Yeast, Brewer's,Baker Yeast,S cerevisiae,Baker's Yeasts,Yeast, Baker
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013438 Sulfhydryl Compounds Compounds containing the -SH radical. Mercaptan,Mercapto Compounds,Sulfhydryl Compound,Thiol,Thiols,Mercaptans,Compound, Sulfhydryl,Compounds, Mercapto,Compounds, Sulfhydryl
D051231 Farnesyltranstransferase An enzyme that catalyzes the synthesis of geranylgeranyl diphosphate from trans, trans-farnesyl diphosphate and isopentenyl diphosphate. Farnesyl Diphosphate-Geranylgeranyl Diphosphate Synthase,Farnesyltransferase,GGDP Synthase,GGPP Synthase,Geranylgeranyl Pyrophosphatase,Geranylgeranyl-Diphosphate Synthase,Farnesyl Diphosphate Geranylgeranyl Diphosphate Synthase,Geranylgeranyl Diphosphate Synthase,Pyrophosphatase, Geranylgeranyl,Synthase, GGDP,Synthase, GGPP,Synthase, Geranylgeranyl-Diphosphate

Related Publications

Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Non-thiol farnesyltransferase inhibitors: N-(4-Acylamino-3-benzoylphenyl)-4-nitrocinnamic acid amides.
February 2002, Bioorganic & medicinal chemistry,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
April 2003, Bioorganic & medicinal chemistry,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity.
January 2005, European journal of medicinal chemistry,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides.
February 2002, Bioorganic & medicinal chemistry letters,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Potent, non-thiol inhibitors of farnesyltransferase.
December 1998, Bioorganic & medicinal chemistry letters,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Non-thiol farnesyltransferase inhibitors: the concept of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.
January 2000, European journal of medicinal chemistry,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Non-thiol farnesyltransferase inhibitors: structure-activity relationships of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.
March 2002, Bioorganic & medicinal chemistry,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Structure-activity relationships of novel anti-malarial agents. Part 6: N-(4-arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
May 2003, Bioorganic & medicinal chemistry letters,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
February 2003, Bioorganic & medicinal chemistry letters,
Andreas Mitsch, and Pia Wissner, and Katrin Silber, and Peter Haebel, and Isabel Sattler, and Gerhard Klebe, and Martin Schlitzer
Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
January 1996, Journal of medicinal chemistry,
Copied contents to your clipboard!