Siavosh Mahboobi

Summary

Affiliation: University of Regensburg
Country: Germany

Publications

  1. doi request reprint Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 53:8546-55. 2010
  2. ncbi request reprint Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents
    S Mahboobi
    Faculty of Chemistry and Pharmacy, Institute of Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 44:4535-53. 2001
  3. doi request reprint Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases
    Siavosh Mahboobi
    Institute of Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 52:2265-79. 2009
  4. ncbi request reprint Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Regensburg, Germany
    Eur J Med Chem 43:1444-53. 2008
  5. ncbi request reprint 2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 50:4405-18. 2007
  6. ncbi request reprint Antibacterial activity of a novel series of 3-bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives--an extended structure-activity relationship study
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    Eur J Med Chem 43:633-56. 2008
  7. ncbi request reprint Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    Bioorg Med Chem 15:2187-97. 2007
  8. ncbi request reprint [4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: synthesis and cytotoxic activity on selected human cancer cell lines
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 49:5769-76. 2006
  9. ncbi request reprint Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 49:3101-15. 2006
  10. ncbi request reprint 3-Bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives as new lead compounds for antibacterially active substances
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    Eur J Med Chem 41:176-91. 2006

Collaborators

Detail Information

Publications16

  1. doi request reprint Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 53:8546-55. 2010
    ..By combining two distinct pharmacologically properties in one molecule, we postulate a broader activity spectrum and less likelihood of drug resistance in cancer patients...
  2. ncbi request reprint Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents
    S Mahboobi
    Faculty of Chemistry and Pharmacy, Institute of Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 44:4535-53. 2001
    ..We conclude, that 2-aroylindoles constitute an interesting new class of antitubulin agents with the potential to be clinically developed for cancer treatment...
  3. doi request reprint Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases
    Siavosh Mahboobi
    Institute of Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 52:2265-79. 2009
    ..Cytotoxicity was evaluated by using a broad panel of tumor cell lines, with selected analogues displaying mean IC(50) values between 3.6 and 7.1 muM...
  4. ncbi request reprint Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Regensburg, Germany
    Eur J Med Chem 43:1444-53. 2008
    ..2 microM; IC(50) Imatinib (1)=0.3 microM). Selectivity hereby seems to be conserved, as shown by the lack of activity on FLT3, a closely related class III receptor tyrosine kinase, which is not affected by the parent compound Imatinib...
  5. ncbi request reprint 2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 50:4405-18. 2007
    ..Comparable to N(1)-hydroxy-N(8)-phenyloctanediamide "2 (SAHA)", cells in the S phase of the cell cycle are depleted, with partial arrest in G1 and G2/M and finally induction of massive apoptosis...
  6. ncbi request reprint Antibacterial activity of a novel series of 3-bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives--an extended structure-activity relationship study
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    Eur J Med Chem 43:633-56. 2008
    ..This might be important in circumventing existing resistance mechanisms. Here we report about the antibacterial activity in an extended structure-activity relationship study...
  7. ncbi request reprint Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    Bioorg Med Chem 15:2187-97. 2007
    ..The loss of one H bond by the NH-O exchange might be partially compensated by, for example, the weak interaction of one furanyl oxygen with FLT3 Cys-828...
  8. ncbi request reprint [4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: synthesis and cytotoxic activity on selected human cancer cell lines
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 49:5769-76. 2006
    ..In depth analysis of the investigated compounds allowed the identification of modifications that altered the pharmacological profile of the compounds from a mitosis-inducing phenotype to a G1 cell cycle arresting phenotype...
  9. ncbi request reprint Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase
    Siavosh Mahboobi
    Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 49:3101-15. 2006
    ..Compound 102 inhibited the proliferation of 32D cells expressing wildtype FLT3 or FLT3-ITD similarly as FLT3 autophosphorylation, and induced apoptosis in primary AML patient blasts...
  10. ncbi request reprint 3-Bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives as new lead compounds for antibacterially active substances
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    Eur J Med Chem 41:176-91. 2006
    ..This might be important in circumventing existing resistance mechanisms. Here we report about the synthesis and on the antibacterial activity in a structure activity relationship study...
  11. ncbi request reprint Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines
    Siavosh Mahboobi
    Department of Pharmaceutical Chemistry I, University of Regensburg, 93040 Regensburg, Germany
    Eur J Med Chem 40:85-92. 2005
    ..As shown by the significant difference in the IC90 values on different tumor cell lines, the investigated compounds seem to act selectively on mammary and renal cancer cells...
  12. ncbi request reprint Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase
    Siavosh Mahboobi
    Faculty of Chemistry and Pharmacy, Institute of Pharmacy, University of Regensburg, D 93040 Regensburg, Germany
    J Med Chem 45:1002-18. 2002
    ....
  13. doi request reprint Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones
    Thomas Beckers
    Department of Pharmaceutical Chemistry I, University of Regensburg, D 93040 Regensburg, Germany
    Bioorg Med Chem 20:125-36. 2012
    ..1-0.3μM for 45. In a panel of 42 human tumor cell lines the sensitivity profile of the novel compounds was shown to be similar to that of the quinazoline class of tyrosine kinase inhibitors lapatinib and erlotinib (Tarceva®)...
  14. ncbi request reprint A single amino acid exchange inverts susceptibility of related receptor tyrosine kinases for the ATP site inhibitor STI-571
    Frank D Bohmer
    Research Unit Molecular Cell Biology, Medical Faculty, Friedrich Schiller University, D 07747 Jena, Germany
    J Biol Chem 278:5148-55. 2003
    ..The binding site models of PDGFR-beta and Flt3 were applied to predict structural approaches for more selective PDGFbeta-receptor inhibitors...
  15. ncbi request reprint 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors
    Thomas Beckers
    ASTA Medica Oncology, D 60314 Frankfurt Main, Germany
    Cancer Res 62:3113-9. 2002
    ..4 days at 400 mg/kg. Therefore, D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources...
  16. pmc The tyrosine kinase FRK/RAK participates in cytokine-induced islet cell cytotoxicity
    Michael Welsh
    Department of Medical Cell Biology, Uppsala University, 75123, Uppsala, Sweden
    Biochem J 382:261-8. 2004
    ..It is concluded that FRK/RAK contributes to cytokine-induced beta-cell death, and inhibition of this kinase could provide means to suppress beta-cell destruction in Type I diabetes...