Publikationen / Publications

Thomas Beckers, Siavosh Mahboobi, Andreas Sellmer, Matthias Winkler, Emerich Eichhorn, Herwig Pongratz, Thomas Ciossek, Thomas Baer, Gerhard Kelter, Heinz-Herbert Fiebig and Mathias Schmidt, Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases, MedChemComm 3, 829-835 (2012).

Thomas Beckers, Andreas Sellmer, Emerich Eichhorn, Herwig Pongratz, Christoph Schächtele, Frank Totzke, Gerhard Kelter, Rebekka Krumbach, Heinz-Herbert Fiebig, Frank-D. Böhmer, Siavosh Mahboobi, 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, Bio. Org. Med. Chem. 20, 125 – 136, (2012).

Siavosh Mahboobi, Andreas Sellmer, Matthias Winkler, Emerich Eichhorn, HerwigPongratz, Thomas Ciossek, Thomas Baer, Thomas Maier and Thomas Beckers, Novel chimeric HDAC inhibitors: A series of Lapatinib hybrides as potent inhibitors of EGFR, erbB-2 and histone deacetylase activity, J.Med.Chem. 53, 8546-8555 (2010).

Uecker, Andrea; Sicker, Marit; Beckers, Thomas; Mahboobi, Siavosh; Haegerstrand, Daniel; Oestman, Arne; Boehmer, Frank-D. Chimeric tyrosine kinase-HDAC inhibitors as antiproliferative agents. Anti-Cancer Drugs (2010), 21(8), 759-765.

Jandt, Enrico; Mutschke, Oliver; Mahboobi, Siavosh; Uecker, Andrea; Platz, Ronny; Berndt, Alexander; Boehmer, Frank-D.; Figulla, Hans R.; Werner, Gerald S. Stent-based release of a selective PDGF-receptor blocker from the bis-indolylmethanon class inhibits restenosis in the rabbit animal model. Vascular Pharmacology (2010), 52(1-2), 55-62.

Romeo, Romagnoli; Pier, Giovanni Baraldi; Maria, Dora Carrion; Olga, Cruz-Lopez; Carlota, Lopez Cara; Giuseppe, Basso; Giampietro, Viola; Mohammed, Khedr; Jan, Balzarini; Siavosh, Mahboobi; Andreas Sellmer; Andrea, Brancale; Ernest, Hamel 2-Arylamino-4-Amino-5-Aroylthiazoles. “One-Pot” Synthesisand Biological Evaluation of a New Class of Inhibitors of Tubulin Polymerization, J. Med. Chem. 52 (17), 5551-5555 (2009).

Heidel, Florian; Lipka, Daniel B.; Mirea, Fian K.; Mahboobi, Siavosh; Grundler, Rebekka; Kancha, Rama K.; Duyster, Justus; Naumann, Michael; Huber, Christoph; Boehmer, Frank D.; Fischer, Thomas. Bis(1H-indol-2-yl)methanones are effective inhibitors of FLT3-ITD tyrosine kinase and partially overcome resistance to PKC412A in vitro. British Journal of Haematology (2009), 144(6), 865-874.

Siavosh Mahboobi, Stefan Dove, Andreas Sellmer, Matthias Winkler, Emerich Eichhorn, Herwig Pongratz, Thomas Ciossek, Thomas Baer, Thomas Maier and Thomas Beckers, 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-Rß and Histone Deacetylases, J. Med. Chem. 52, 2265-2279 (2009).

Siavosh Mahboobi, Andreas Sellmer, Asma Eswayah, Sigurd Elz, Andrea Uecker, Frank-D. Böhmer, Inhibition of PDGFR tyrosine kinase avtivity 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 Eur. J. Med. Chem. 43(7), 633-656 (2008).

Siavosh Mahboobi, Emerich Eichhorn, Matthias Winkler, Andreas Sellmer, Ute Möllmann, Antibacterial Activity of a Novel Series of 3-Bromo-4-(1H-3-indolyl)-2,5-dihydro-1H2,5-pyrroledione derivatives – An extended structure activity relationship study Eur. J. Med. Chem. 43(3), 633-656 (2008).

Siavosh Mahboobi, Andreas Sellmer, Heymo Höcher, Christian Garhammer, Herwig Pongratz, Thomas Maier , Thomas Ciossek and Thomas Beckers 2-Aroylindoles and 2-Aroylbenzofurans with N hydroxyacrylamide substructures as novel series of rationally designed HDAC inhibitors, J. Med. Chem. 50, 4405-4418, (2007).

Siavosh Mahboobi, Andrea Uecker, Christophe Cénac, Andreas Sellmer, Emerich Eichhorn, Sigurd Elz, Frank-D. Böhmer and Stefan Dove, Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones, Bio. Org. Med. Chem. 15, 2187-2197, (2007).

Siavosh Mahboobi, Andreas Sellmer, Heymo Höcher, Emerich Eichhorn, Thomas Bär, Mathias Schmidt, Thomas Maier, Josef F. Stadlwieser, Thomas L. Beckers [4-(Imidazol-1-yl)-thiazol-2-yl]phenylamines – A novel class of highly potent colchicine site binding tubulin polymerization inhibitors: Synthesis and cytotoxic activity on some human cancer cell lines, J. Med. Chem. 49, 5769-5776, (2006).

Mahboobi S., Uecker A., Sellmer A., Cénac C., Höcher H., Pongratz H., Eichhorn E., Hufsky H., Trümpler A., Sicker M., Heidel F., Fischer T., Stocking C., Elz S., Böhmer F.D., and Dove S. Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase, J. Med. Chem. 49, 3101-3115, (2006).

Mahboobi. S., Sellmer, A. and Beckers, T. Development of Tubulin Inhibitors as Antimitotic Agents for Cancer Therapy, Studies in Natural Products Chemistry, 33, 719-750, (2006).

Siavosh Mahboobi, Emerich Eichhorn, Alfred Popp, Andreas Sellmer, Sigurd Elz and Ute Möllmann, 3-Bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione Derivatives as New Lead Compounds for Antibacterially Active Substances, Eur. J. Med. Chem. 41, 176-191, (2006).

Mahboobi, Siavosh; Sellmer, Andreas; Eichhorn, Emerich; Beckers, Thomas; Fiebig, Heinz-Herbert; Kelter, Gerhard. Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines. Eur. J. Med. Chem. 40, 85-92, (2005).

Ralf Freund, Siavosh Mahboobi, Klaus Noak, Peter Schönholzer and Karl Bernauer, Diastereoselective Spirocyclization of C-(Alkyloxycarbonyl)formimines of 2-Substituted 1H-Indole-3-ethanamines (= Tryptamines): Basic Studies, Helv. Chim. Acta 88, 3274-3275 (2005).

Mahboobi, S.; Sellmer, A.; Burgemeister, Th.; Lyssenko, A.; Schollmeyer, D. Synthesis of Naturally Occuring Pyrazine and Imidazol Alkaloids from Botryllus Leachi, Monatshefte für Chemie, 135, 333-342, (2004).

Welsh, M.; Welsh, C.; Ekmann, M.; Dixelius, J.; Haegerkvist, R.; Anneren, C.; Akerblum, B.; Mahboobi, S.; Charndrasekhavan, S.; Liu, E.T. The tyrosine kinase FRK/RAK Participates in cytokine-induced islet cell cytotoxicity, Biochem. J. 382(1), 261-268, (2004)

Beckers, Th.; Mahboobi, S.; Natural, semisynthetic and synthetic microtubule inhibitors of cancer therapy; Drug of the Future 28(8), 767-785, (2003) - Review-Artikel.

Frank D. Böhmer, Luchezar Karagyozov, Andrea Uecker, Hubert Serve, Alexander Botzki, Siavosh Mahboobi and Stefan Dove. A single amino acid exchange inverts susceptibility of related receptor tyrosine kinases for the ATP-site inhibitor STI-571. J. Biol. Chem. 278, 5148-5155 (2003).

Beckers, T.; Reissmann, T.; Schmidt, M.; Burger, A.; Fiebig, H.H.; Vanhoefer, U.; Pongratz, H.; Hufsky, H.; Hockemeyer, Jörg,; Frieser, M.; Mahboobi, S. 2-Aroylindoles, a Novel Class of Potent, Orally Active Small Molecule Tubulin Inhibitors Cancer Res.; 62, 3113-3119 (2002).

Teller S., Krämer D.; Böhmer S-A.; Tse K.F.; Small D.; Mahboobi S.; Wallrapp C.; Beckers T.; Kratz-Albers K.; Schwäble J., Serve H.; Böhmer F-D.; Bis(1H-2-indolyl)-1-methanones as inhibitors of the hematopoietic tyrosine kinase Flt3. Leukemia 1528-1534 (2002).

S. Mahboobi, S. Teller, H. Pongratz, H. Hufsky, A. Sellmer, A. Botzki, A. Uecker, T. Beckers, S. Baasner, C. Schächtele, F. Überall, M. U. Kassack, S. Dove, F.-D. Böhmer, Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet derived growth factor receptor kinase, J. Med Chem.; 45, 1002-1018 (2002).

Mahboobi, S.; Pongratz, H.; Hufsky, H.; Hockemeyer, J.; Frieser, M.; Lyssenko, A.; Paper, D.H.; Bürgermeister, J.; Böhmer, F.-D.; Fiebig, H.-H.; Burger, A.; Baasner, S.; Beckers, T. Synthetic 2-Aroylindole Derivatives as a New Class of Potent Tubulin Inhibitory, Antimitotic Agents. J. Med. Chem.; 44, 4535-4553 (2001).

S. Mahboobi, S. Eluwa, M. Koller, A. Popp, D. Schollmeyer, Synthesis of Pyrrolo(3´,4´: 2,3)azepino(4,5,6-cd)indole-8,10-diones, J. Heterocycl. Chem.; 37, 1177 (2000).

S. Teller, S. Eluwa, M. Koller, A. Uecker, T. Beckers, S. Baasner, F.-D. Böhmer, S. Mahboobi, Pyrrolo(3,4-c)-β-carboline-diones as a novel class of inhibitors of the plateletderived growth factor receptor kinase, Eur. J. Med. Chem.; 35, 413 (2000).

S. Mahboobi, I. Dechant, H. Reindl, H. Pongratz, A. Popp, D. Schollmeyer Synthesis of Bis(indolylmaleimide) Macrocycles, J. Heterocycl. Chem., 37, 307 (2000).

S. Mahboobi, M. Koller, D. Schollmeyer, Synthesis of the Racemates of the β-Carboline Alkaloid Chrysotricine and ist Diastereomer, Monatsh. Chem. 131, 383 (2000).

S. Mahboobi, S. Dove, S. Kuhr, A. Popp, Homo-Arcyriaflavin: The Synthesis of Ring expanded Arcyriaflavin Analogs, J. Org. Chem, 64, 8130 (1999).

S. Mahboobi, E. Eibler, M. Koller, S. K. KC , A. Popp, D. Schollmeyer, Synthesis of Pyrrolidin-2-ones and of Staurosporine-Aglycon (K-252c) by Intermolecular Michael Reaction, J. Org. Chem, 64, 4697 (1999).

S. Mahboobi, S. Dove, H. Pongratz, S. Kuhr, Synthesis of Arcyriarubine Regioisomers by Pd(0)-Catalysis or via Lithiated Indole Derivatives - Conformational Analysis by Semiempirical and X-Ray Methods, Pharmazie, Pharmazie, 54, 820 (1999).

S. Mahboobi, S. Eluwa, S. K. K.C. M. Koller, K. Störl, β-Carbolinedione Derivatives as Topoisomerase Inhibitors, Arch. Pharm, Pharm. Med. Chem. 332, 249 (1999).

S. Mahboobi, W. Wiegrebe, A. Popp, First Synthesis of Enantiomerically Pure-(-)-(S)-Brevicolline, J. Nat. Prod, 62, 577 (1999).

S. Mahboobi, A. Popp, W.F. Fleck, Synthesis and biological evaluation of 4,4-Dimethyl-5,5 di(1-methylethyl)-2,3,4,5-tetrahydro-1H-dipyrrolo[3,4-d:2,1-f] [1,2]azasiline-1,3-dione and other Pyrrolediones as new antibacterial active agents, Pharmazie, 54, 730 (1999).

S. Mahboobi, H. Pongratz, Synthesis of 2´-Amino-3´-methoxyflavone (PD 98059), Synth. Commun., 29(10), 1645 (1999).

S. Mahboobi, A. Popp, T. Burgemeister, D. Schollmeyer, Diastereoselective synthesis of (-)-1-methyl-(3S,4R)-3,4-bis((2S)-N-(tert-butyloxycarbonyl)pyrrolidin-2-yl)-2-pyrrolidinone by an asymmetric Michael reaction, Tetrahedron Asymm., 9, 2369 (1998).

S. Mahboobi, S. Kuhr, S. Dove, P. J. Bednarski, T. Burgemeister, D. Schollmeyer, X-Ray crystal structure of Woodinin and Conformational Analysis by Semiempirical and 1H-NMR Methods, J. Nat. Prod., 60, 587 (1997).

S. Mahboobi, H.Pongratz, W. Wiegrebe, Preparation of the alkaloid setigerine,Pharmazie 52, 399 (1997). S. Mahboobi, K. Hahn, K. Mayer, W. Wiegrebe, M. Ertan, Structure of the Alkaloid Nazlinin, Sci. Pharm. 64, 565 ( 1996).

S. Mahboobi, S. Kuhr, M. Koller, Synthesis of Carbazole Derivatives, III Synthesis of new Pyrrolidino[3,4-c]carbazoles by intramolecular Michael Addition Tetrahedron 52, 6373-6382 (1996).

S.Mahboobi, W.Wagner and Thomas Burgemeister, Syntheses of (RS )- and (S)- (-) Nazlinin and (RS)- and (+)-6-Azacyclodeca[5,4-b]indol-1-amine, Arch. Pharm. (Weinheim) 328, 371-376 (1995).

S.Mahboobi, S.Kuhr, Synthese von Carbazolderivaten, 2. Mitt.: 2-Substituierte Indole als Zwischenprodukte von Pyrrolo[3,4-c]carbazolen, Arch. Pharm. (Weinheim) 328, 45-52 (1995).

S.Mahboobi, Th.Burgemeister, F.Kastner, Synthese von Carbazolderivaten, 1. Mitt.: Über die Reaktion von 3-(2-Nitroethenyl)indol-2-malonestern mit Michael-Akzeptoren, Arch. Pharm. (Weinheim) 328, 29-38 (1995).

S.Mahboobi, S.Kuhr, W.Meindl, Antimykobakteriell wirksame Carbazolderivat, Arch. Pharm. (Weinheim) 327, 611-617 (1994).

S.Mahboobi, G.Grothus, E.von Angerer, 3-Substituierte 2-Phenylindole: Synthese und biologische Eigenschaften, Arch. Pharm. (Weinheim) 327, 481-492 (1994).

S.Mahboobi, W.Wagner, Th.Burgemeister, W.Wiegrebe, Non-Identity of Nazlinin and 6-Azacyclodeca[5,4-b]indol-1-amine, Arch. Pharm. (Weinheim) 327, 463-465 (1994).

S.Mahboobi, A.Karcher, G.Grothus, W.Wagner, W.Wiegrebe, Removal of an Cyclic Amine Substituent by Dehydrogenation of 4-Substituted 3,4-Dihydro- and 1,2,3,4 Tetrahydroisoquinolines, Arch.Pharm. (Weinheim) 327, 417-428 (1994).

S.Mahboobi, G.Grothus, 1,3-Dinitropropane als Vorstufen von 1,3-Diaminopropanen, Arch. Pharm. (Weinheim) 327, 349-358 (1994).

S.Mahboobi, G.Grothus, W.Meindl, Antimykobakteriell wirksame Indolderivate, Arch. Pharm. (Weinheim) 327, 105-114 (1994).

S.Mahboobi, Th.Burgemeister, W.Wiegrebe, Woodinine and its Stereomers - Absolute Configuration, Arch. Pharm. (Weinheim) 326, 33-37 (1993).

S.Mahboobi, Synthesis of the Alkaloid Woodinine, Arch. Pharm. (Weinheim) 325, 249-250 (1992).

S.Mahboobi, E.Seidl, E.Eibler, W.Wiegrebe, Removal of the Pyrrolidine Group by Dehydrogenation of a 4-Pyrrolidin-2-yl-tetrahydroisoquinoline, Arch.Pharm. (Weinheim) 325, 679-683 (1992).

S.Mahboobi, W.Wiegrebe, Synthesis of the Preininger-Alkaloid and its Enantioselective Reduction to Macrostomine, Arch.Pharm. (Weinheim) 324, 275-281 (1991).

R. Freund, S.Mahboobi, K.Noak, P.Schönholzer, K.Bernauer, Diastereoselective Spirocyclization of C-(Alkyloxycarbonyl)formimines of 2-Substituted 1H-Indole-3- ethanamines (= Tryptamines): Basic Studies, Helv.Chim. Acta 73, 439-454 (1990).

S.Mahboobi, K.Bernauer, Synthesis of Esters of 3-(2-Aminoethyl)-1H-indole-2-acetic Acid and 3-(2-Aminoethyl)-1H-indole-2-malonic Acid (= 2-[3-(2-Aminoethyl)-1H-indol-2-yl]propanedioic Acid), Helv.Chim. Acta 71, 2034-2041 (1988).

S.Mahboobi, E.Chr.Fischer, E.Eibler,W.Wiegrebe, Preparation and GC-MS Identification of N-Methyl-Δ3-pyrroline, Arch.Pharm. (Weinheim) 321, 423-424, (1988).

S.Mahboobi, W.Wiegrebe, Enantioselective Synthesis of some Nicotiana Alkaloids, Arch.Pharm. (Weinheim) 321, 175-177 (1988).

H.Brunner, A.Kürzinger, S.Mahboobi, W.Wiegrebe, Enantioselective Hydrosilylation and Hydrogenation of Alkaloid Precursors, Arch.Pharm. (Weinheim) 321, 73-76 (1988).

R.Becker, H.Brunner, S.Mahboobi, W.Wiegrebe, Enantioselektive Synthese von prochiralen 3,4-Dihydro-2H-pyrrol-Derivaten, Angew.Chem. 97, 969-970, (1985).

W.Wiegrebe, S.Mahboobi, G.Dannhardt, K.K.Mayer, E.Eibler, Synthesis of (+/-)- Macrostomine, Chimia 35, 288-289 (1981).

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