Peter Nussbaumer

Summary

Country: Germany

Publications

  1. doi request reprint Medicinal Chemists of the 21(st) Century--Who Are We and Where to Go?
    Peter Nussbaumer
    Lead Discovery Center GmbH, Otto Hahn Straße 15, 44227 Dortmund Germany
    ChemMedChem 10:1133-9. 2015
  2. doi request reprint Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1230 Vienna, Austria
    Bioorg Med Chem 16:7552-60. 2008
  3. ncbi request reprint Synthesis and immobilization of erythro-C14-omega-aminosphingosine-1-phosphate as a potential tool for affinity chromatography
    Thomas Ullrich
    Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1230 Wien, Austria
    ChemMedChem 3:356-60. 2008
  4. doi request reprint Phosphorylation by sphingosine kinase 2 is essential for in vivo potency of FTY720 analogues
    Klemens Högenauer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1235 Wien, Austria
    ChemMedChem 3:1027-9. 2008
  5. ncbi request reprint NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies
    Peter Ettmayer
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1230 Vienna, Austria
    Bioorg Med Chem Lett 16:84-7. 2006
  6. ncbi request reprint N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
    Philipp Lehr
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1235 Vienna, Austria
    Bioorg Med Chem Lett 15:1235-8. 2005
  7. ncbi request reprint 6-[2-(adamantylidene)-hydroxybenzoxazole]-O-sulfamate, a steroid sulfatase inhibitor for the treatment of androgen- and estrogen-dependent diseases
    Andreas Billich
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    J Steroid Biochem Mol Biol 92:29-37. 2004
  8. ncbi request reprint An efficient, one-pot synthesis of various ceramide 1-phosphates from sphingosine 1-phosphate
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    Chem Phys Lipids 151:125-8. 2008
  9. ncbi request reprint Steroid sulfatase inhibitors: their potential in the therapy of breast cancer
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    Curr Med Chem Anticancer Agents 5:507-28. 2005
  10. ncbi request reprint 2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase
    Amarylla Horvath
    Novartis Institute for BioMedical Research Vienna, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 47:4268-76. 2004

Collaborators

Detail Information

Publications21

  1. doi request reprint Medicinal Chemists of the 21(st) Century--Who Are We and Where to Go?
    Peter Nussbaumer
    Lead Discovery Center GmbH, Otto Hahn Straße 15, 44227 Dortmund Germany
    ChemMedChem 10:1133-9. 2015
    ..By providing my opinion on these aspects, I hope to stimulate discussions and change within the community...
  2. doi request reprint Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1230 Vienna, Austria
    Bioorg Med Chem 16:7552-60. 2008
    ..Moreover, we established structure-activity relationships for the effect of modifications in the 2,5-dimethoxyphenyl moiety ("ring A") of the molecule on in vitro antiproliferative activity...
  3. ncbi request reprint Synthesis and immobilization of erythro-C14-omega-aminosphingosine-1-phosphate as a potential tool for affinity chromatography
    Thomas Ullrich
    Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1230 Wien, Austria
    ChemMedChem 3:356-60. 2008
    ..Finally, the omega-amino intermediate is immobilized on an affinity matrix. The choice of a UV-active phosphate protecting group allows for quantification of resin loading after cleavage which amounted to 66 %...
  4. doi request reprint Phosphorylation by sphingosine kinase 2 is essential for in vivo potency of FTY720 analogues
    Klemens Högenauer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1235 Wien, Austria
    ChemMedChem 3:1027-9. 2008
  5. ncbi request reprint NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies
    Peter Ettmayer
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1230 Vienna, Austria
    Bioorg Med Chem Lett 16:84-7. 2006
    ..Furthermore, the NBD-(R)-AAL phosphates 10c,d were proven to be a functional S1P receptor agonist...
  6. ncbi request reprint N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
    Philipp Lehr
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1235 Vienna, Austria
    Bioorg Med Chem Lett 15:1235-8. 2005
    ....
  7. ncbi request reprint 6-[2-(adamantylidene)-hydroxybenzoxazole]-O-sulfamate, a steroid sulfatase inhibitor for the treatment of androgen- and estrogen-dependent diseases
    Andreas Billich
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    J Steroid Biochem Mol Biol 92:29-37. 2004
    ..Based on these data, clinical studies with AHBS in acne patients are warranted, in order to verify the hypothesis on the importance of the sulfatase pathway in androgen-dependent skin diseases...
  8. ncbi request reprint An efficient, one-pot synthesis of various ceramide 1-phosphates from sphingosine 1-phosphate
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    Chem Phys Lipids 151:125-8. 2008
    ..Thus, ceramide 1-phosphates with various fatty acid chains and with fluorescent and affinity labels attached to the sphingoid backbone were prepared in good yields...
  9. ncbi request reprint Steroid sulfatase inhibitors: their potential in the therapy of breast cancer
    Peter Nussbaumer
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, A 1235 Vienna, Austria
    Curr Med Chem Anticancer Agents 5:507-28. 2005
    ..In particular, these agents featuring an extended mode of action hold promise to be included in the armamentarium to fight endocrine-dependent cancer...
  10. ncbi request reprint 2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase
    Amarylla Horvath
    Novartis Institute for BioMedical Research Vienna, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 47:4268-76. 2004
    ..Compound 5j is an example of a reversible STS inhibitor with potent activity toward the target enzyme in a cellular test system. Moreover, 5d,j are stable and have no estrogenic potential...
  11. ncbi request reprint Synthesis of borondipyrromethene (BODIPY)-labeled sphingosine derivatives by cross-metathesis reaction
    Carsten Peters
    Novartis Institutes for BioMedical Research, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Org Chem 72:1842-5. 2007
    ..One of these derivatives (11d) was identified as the first reported selective substrate for SPHK-1...
  12. ncbi request reprint Regulation and traffic of ceramide 1-phosphate produced by ceramide kinase: comparative analysis to glucosylceramide and sphingomyelin
    Alistair Boath
    Novartis Institutes for BioMedical Research, Vienna, Brunnerstrasse 59, Wien, Austria
    J Biol Chem 283:8517-26. 2008
    ....
  13. ncbi request reprint Medicinal chemistry aspects of drug targets in sphingolipid metabolism
    Peter Nussbaumer
    Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1235 Vienna, Austria
    ChemMedChem 3:543-51. 2008
  14. ncbi request reprint Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase
    Peter Nussbaumer
    Novartis Research Institute Vienna, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 46:5091-4. 2003
    ..Compound 2g, which lacks estrogenicity while potently inhibiting STS, has an ideal in vitro profile for the treatment of breast cancer...
  15. ncbi request reprint Fluorescence-labeled sphingosines as substrates of sphingosine kinases 1 and 2
    Peter Ettmayer
    Novartis Institute for Biomedical Research, Brunnerstrasse 59, Vienna A 1235, Austria
    Bioorg Med Chem Lett 14:1555-8. 2004
    ....
  16. ncbi request reprint 2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase
    Peter Nussbaumer
    Novartis Research Institute Vienna, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 45:4310-20. 2002
    ..As with 1, all chromenone sulfamates are irreversible inhibitors of STS with a biphasic time course of inactivation...
  17. ncbi request reprint 4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase
    Peter Nussbaumer
    Novartis Research Institute, Brunnerstrasse 59, A 1235, Vienna, Austria
    Bioorg Med Chem Lett 12:2093-5. 2002
    ..With an IC(50) value of 190 nM the 4,4'-derivative is the first small monocyclic STS inhibitor coming close to the potency of the steroidal standard estrone sulfamate...
  18. ncbi request reprint Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase
    Peter Nussbaumer
    Novartis Research Institute Vienna, Brunnerstrasse 59, A 1235 Vienna, Austria
    Bioorg Med Chem Lett 13:3673-7. 2003
    ..Mechanistic investigations revealed that the compounds are reversible, competitive inhibitors of STS...
  19. ncbi request reprint Inhibitors of vitamin D hydroxylases: structure-activity relationships
    Inge Schuster
    Institute of Pharmaceutical Chemistry, University Vienna, Althanstrasse 15, A 1090 Wien, Osterreich
    J Cell Biochem 88:372-80. 2003
    ..In the absence of crystal structures, our inhibitors are valuable tools to model and understand the active sites of vitamin D hydroxylases, resulting in the design of powerful, selective therapeutics...
  20. ncbi request reprint LAV694, a new antiproliferative agent showing improved skin tolerability vs. clinical standards for the treatment of actinic keratosis
    Jesus Medina
    Preclinical Safety Department, Novartis Pharma AG, WSH 2881 P03, CH 4002 Basel, Switzerland
    Biochem Pharmacol 66:1885-95. 2003
    ..This resulted in an improved skin tolerability in comparison with 5-FU and podophyllotoxin...
  21. ncbi request reprint Steroid sulfatase inhibitors
    Peter Nussbaumer
    Novartis Institutes for Biomedical Research Vienna, Brunner Strasse 59, A 1235 Vienna, Austria
    Med Res Rev 24:529-76. 2004
    ..The recent publication of the X-ray structure of STS will further boost research activities on this attractive target...