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Items: 1 to 50 of 65

1.

Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy.

Manley PW, Caravatti G, Furet P, Roesel J, Tran P, Wagner T, Wartmann M.

Biochemistry. 2018 Sep 25;57(38):5576-5590. doi: 10.1021/acs.biochem.8b00727. Epub 2018 Sep 13.

PMID:
30148617
2.

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Jeay S, Ferretti S, Holzer P, Fuchs J, Chapeau EA, Wartmann M, Sterker D, Romanet V, Murakami M, Kerr G, Durand EY, Gaulis S, Cortes-Cros M, Ruetz S, Stachyra TM, Kallen J, Furet P, Würthner J, Guerreiro N, Halilovic E, Jullion A, Kauffmann A, Kuriakose E, Wiesmann M, Jensen MR, Hofmann F, Sellers WR.

Cancer Res. 2018 Nov 1;78(21):6257-6267. doi: 10.1158/0008-5472.CAN-18-0338. Epub 2018 Aug 22.

PMID:
30135191
3.

N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.

Schlapbach A, Revesz L, Pissot Soldermann C, Zoller T, Régnier CH, Bornancin F, Radimerski T, Blank J, Schuffenhauer A, Renatus M, Erbel P, Melkko S, Heng R, Simic O, Endres R, Wartmann M, Quancard J.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2153-2158. doi: 10.1016/j.bmcl.2018.05.017. Epub 2018 May 9.

PMID:
29759726
4.

Continuous low-dose infusion of patupilone increases the therapeutic index in mouse and rat tumour models.

Becquet M, Laborde L, Texier C, Sterker D, Gschwind HP, Pfaar U, Wartmann M, O'Reilly TM, McSheehy PM.

Anticancer Drugs. 2018 Aug;29(7):691-701. doi: 10.1097/CAD.0000000000000639.

PMID:
29734209
5.

2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.

Knoepfel T, Furet P, Mah R, Buschmann N, Leblanc C, Ripoche S, Graus-Porta D, Wartmann M, Galuba I, Fairhurst RA.

ACS Med Chem Lett. 2018 Feb 1;9(3):215-220. doi: 10.1021/acsmedchemlett.7b00485. eCollection 2018 Mar 8.

PMID:
29541363
6.

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.

J Med Chem. 2016 Jan 14;59(1):132-46. doi: 10.1021/acs.jmedchem.5b01582. Epub 2015 Dec 21.

PMID:
26629594
7.

CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors.

Vora SR, Juric D, Kim N, Mino-Kenudson M, Huynh T, Costa C, Lockerman EL, Pollack SF, Liu M, Li X, Lehar J, Wiesmann M, Wartmann M, Chen Y, Cao ZA, Pinzon-Ortiz M, Kim S, Schlegel R, Huang A, Engelman JA.

Cancer Cell. 2014 Jul 14;26(1):136-49. doi: 10.1016/j.ccr.2014.05.020. Epub 2014 Jul 4.

8.

The tyrosine phosphatase PTPN14 is a negative regulator of YAP activity.

Michaloglou C, Lehmann W, Martin T, Delaunay C, Hueber A, Barys L, Niu H, Billy E, Wartmann M, Ito M, Wilson CJ, Digan ME, Bauer A, Voshol H, Christofori G, Sellers WR, Hofmann F, Schmelzle T.

PLoS One. 2013 Apr 16;8(4):e61916. doi: 10.1371/journal.pone.0061916. Print 2013.

9.

Acentrosomal spindle organization renders cancer cells dependent on the kinesin HSET.

Kleylein-Sohn J, Pöllinger B, Ohmer M, Hofmann F, Nigg EA, Hemmings BA, Wartmann M.

J Cell Sci. 2012 Nov 15;125(Pt 22):5391-402. doi: 10.1242/jcs.107474. Epub 2012 Sep 3.

10.

Anti-cancer activity of 5-O-alkyl 1,4-imino-1,4-dideoxyribitols.

Bello C, Dal Bello G, Cea M, Nahimana A, Aubry D, Garuti A, Motta G, Moran E, Fruscione F, Pronzato P, Grossi F, Patrone F, Ballestrero A, Dupuis M, Sordat B, Zimmermann K, Loretan J, Wartmann M, Duchosal MA, Nencioni A, Vogel P.

Bioorg Med Chem. 2011 Dec 15;19(24):7720-7. doi: 10.1016/j.bmc.2011.07.053. Epub 2011 Jul 30.

PMID:
22079865
11.

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D.

J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222. Epub 2011 Sep 21.

PMID:
21936542
12.

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F.

Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22.

13.

Natural products as leads for anticancer drug discovery: discovery of new chemotypes of microtubule stabilizers through reengineering of the epothilone scaffold.

Altmann KH, Cachoux F, Feyen F, Gertsch J, Kuzniewski CN, Wartmann M.

Chimia (Aarau). 2010;64(1-2):8-13.

PMID:
21137676
14.

Evaluation of the mTOR inhibitor, everolimus, in combination with cytotoxic antitumor agents using human tumor models in vitro and in vivo.

O'Reilly T, McSheehy PM, Wartmann M, Lassota P, Brandt R, Lane HA.

Anticancer Drugs. 2011 Jan;22(1):58-78. doi: 10.1097/CAD.0b013e3283400a20.

PMID:
20890178
15.

Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.

Manley PW, Stiefl N, Cowan-Jacob SW, Kaufman S, Mestan J, Wartmann M, Wiesmann M, Woodman R, Gallagher N.

Bioorg Med Chem. 2010 Oct 1;18(19):6977-86. doi: 10.1016/j.bmc.2010.08.026. Epub 2010 Aug 14.

PMID:
20817538
16.

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T.

Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29.

17.

Extended kinase profile and properties of the protein kinase inhibitor nilotinib.

Manley PW, Drueckes P, Fendrich G, Furet P, Liebetanz J, Martiny-Baron G, Mestan J, Trappe J, Wartmann M, Fabbro D.

Biochim Biophys Acta. 2010 Mar;1804(3):445-53. doi: 10.1016/j.bbapap.2009.11.008. Epub 2009 Nov 14.

PMID:
19922818
18.

The Ret receptor tyrosine kinase pathway functionally interacts with the ERalpha pathway in breast cancer.

Boulay A, Breuleux M, Stephan C, Fux C, Brisken C, Fiche M, Wartmann M, Stumm M, Lane HA, Hynes NE.

Cancer Res. 2008 May 15;68(10):3743-51. doi: 10.1158/0008-5472.CAN-07-5100.

19.

Total synthesis of hypermodified epothilone analogs with potent in vitro antitumor activity.

Kuzniewski CN, Gertsch J, Wartmann M, Altmann KH.

Org Lett. 2008 Mar 20;10(6):1183-6. doi: 10.1021/ol800089x. Epub 2008 Feb 28.

PMID:
18303900
20.

Pharmacokinetic profile of the microtubule stabilizer patupilone in tumor-bearing rodents and comparison of anti-cancer activity with other MTS in vitro and in vivo.

O'Reilly T, Wartmann M, Brueggen J, Allegrini PR, Floersheimer A, Maira M, McSheehy PM.

Cancer Chemother Pharmacol. 2008 Nov;62(6):1045-54. doi: 10.1007/s00280-008-0695-9. Epub 2008 Feb 27.

PMID:
18301895
21.

Epothilones as lead structures for the synthesis-based discovery of new chemotypes for microtubule stabilization.

Feyen F, Cachoux F, Gertsch J, Wartmann M, Altmann KH.

Acc Chem Res. 2008 Jan;41(1):21-31. Epub 2007 Dec 27. Review.

PMID:
18159935
22.

The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells.

Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R, Caravatti G, Fabbro D, Lane HA, Fagin JA.

Cancer Res. 2007 Jul 15;67(14):6956-64.

23.

Total synthesis and biological evaluation of a C(10)/C(12)-phenylene-bridged analog of epothilone D.

End N, Furet P, van Campenhout N, Wartmann M, Altmann KH.

Chem Biodivers. 2004 Nov;1(11):1771-84.

PMID:
17191815
24.

Molecular design and chemical synthesis of a highly potent epothilone.

Nicolaou KC, Pratt BA, Arseniyadis S, Wartmann M, O'Brate A, Giannakakou P.

ChemMedChem. 2006 Jan;1(1):41-4. No abstract available.

PMID:
16892332
25.

Structure-activity relationships in side-chain-modified epothilone analogues--how important is the position of the nitrogen atom?

Bold G, Wojeik S, Caravatti G, Lindauer R, Stierlin C, Gertsch J, Wartmann M, Altmann KH.

ChemMedChem. 2006 Jan;1(1):37-40. No abstract available.

PMID:
16892331
26.

Design and synthesis of 12-aza-epothilones (azathilones)--"non-natural" natural products with potent anticancer activity.

Feyen F, Gertsch J, Wartmann M, Altmann KH.

Angew Chem Int Ed Engl. 2006 Sep 4;45(35):5880-5. No abstract available.

PMID:
16871640
27.

Total synthesis and biological assessment of benzimidazole-based analogues of epothilone A: ambivalent effects on cancer cell growth inhibition.

Cachoux F, Isarno T, Wartmann M, Altmann KH.

Chembiochem. 2006 Jan;7(1):54-7. No abstract available.

PMID:
16345113
28.

Patupilone induced vascular disruption in orthotopic rodent tumor models detected by magnetic resonance imaging and interstitial fluid pressure.

Ferretti S, Allegrini PR, O'Reilly T, Schnell C, Stumm M, Wartmann M, Wood J, McSheehy PM.

Clin Cancer Res. 2005 Nov 1;11(21):7773-84.

29.

Scaffolds for microtubule inhibition through extensive modification of the epothilone template.

Cachoux F, Isarno T, Wartmann M, Altmann KH.

Angew Chem Int Ed Engl. 2005 Dec 1;44(45):7469-73. No abstract available.

PMID:
16240301
30.

Patupilone (epothilone B, EPO906) inhibits growth and metastasis of experimental prostate tumors in vivo.

O'Reilly T, McSheehy PM, Wenger F, Hattenberger M, Muller M, Vaxelaire J, Altmann KH, Wartmann M.

Prostate. 2005 Nov 1;65(3):231-40.

PMID:
15948135
31.

Patupilone acts as radiosensitizing agent in multidrug-resistant cancer cells in vitro and in vivo.

Hofstetter B, Vuong V, Broggini-Tenzer A, Bodis S, Ciernik IF, Fabbro D, Wartmann M, Folkers G, Pruschy M.

Clin Cancer Res. 2005 Feb 15;11(4):1588-96.

32.

Patupilone (epothilone B, EPO906) and imatinib (STI571, Glivec) in combination display enhanced antitumour activity in vivo against experimental rat C6 glioma.

O'Reilly T, Wartmann M, Maira SM, Hattenberger M, Vaxelaire J, Muller M, Ferretti S, Buchdunger E, Altmann KH, McSheehy PMJ.

Cancer Chemother Pharmacol. 2005 Apr;55(4):307-317. doi: 10.1007/s00280-004-0913-z. Epub 2004 Oct 26.

PMID:
15723258
33.

Biomimetic total synthesis of gambogin and rate acceleration of pericyclic reactions in aqueous media.

Nicolaou KC, Xu H, Wartmann M.

Angew Chem Int Ed Engl. 2005 Jan 21;44(5):756-61. No abstract available.

PMID:
15657969
34.

Psychosocial impact of living-related kidney transplantation on donors and partners.

Neuhaus TJ, Wartmann M, Weber M, Landolt MA, Laube GF, Kemper MJ.

Pediatr Nephrol. 2005 Feb;20(2):205-9. Epub 2004 Dec 31.

PMID:
15627165
35.

Patupilone (epothilone B) inhibits growth and survival of multiple myeloma cells in vitro and in vivo.

Lin B, Catley L, LeBlanc R, Mitsiades C, Burger R, Tai YT, Podar K, Wartmann M, Chauhan D, Griffin JD, Anderson KC.

Blood. 2005 Jan 1;105(1):350-7. Epub 2004 Sep 14.

36.

AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.

Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J, Meyer T, Tang C, Wartmann M, Wood J, Caravatti G.

Cancer Res. 2004 Jul 15;64(14):4931-41.

37.

4. The natural products epothilones A and B as lead structures for anticancer drug discovery: chemistry, biology, and SAR studies.

Altmann KH, Flörsheimer A, O'Reilly T, Wartmann M.

Prog Med Chem. 2004;42:171-205. Review. No abstract available.

PMID:
15003721
38.

STI571 enhances the therapeutic index of epothilone B by a tumor-selective increase of drug uptake.

Pietras K, Stumm M, Hubert M, Buchdunger E, Rubin K, Heldin CH, McSheehy P, Wartmann M, Ostman A.

Clin Cancer Res. 2003 Sep 1;9(10 Pt 1):3779-87.

39.

Design, synthesis, and biological properties of highly potent epothilone B analogues.

Nicolaou KC, Sasmal PK, Rassias G, Reddy MV, Altmann KH, Wartmann M, O'Brate A, Giannakakou P.

Angew Chem Int Ed Engl. 2003 Aug 4;42(30):3515-20. No abstract available.

PMID:
12900969
40.

EPO906 (epothilone B): a promising novel microtubule stabilizer.

Rothermel J, Wartmann M, Chen T, Hohneker J.

Semin Oncol. 2003 Jun;30(3 Suppl 6):51-5. Review.

PMID:
12802795
41.

The biology and medicinal chemistry of epothilones.

Wartmann M, Altmann KH.

Curr Med Chem Anticancer Agents. 2002 Jan;2(1):123-48. Review.

PMID:
12678754
42.

Synthesis, conformational analysis, and bioassay of 9,10-didehydroepothilone D.

White JD, Sundermann KF, Wartmann M.

Org Lett. 2002 Mar 21;4(6):995-7.

PMID:
11893205
44.

Synthesis and biological evaluation of aza-epothilones.

Schinzer D, Altmann KH, Stuhlmann F, Bauer A, Wartmann M.

Chembiochem. 2000 Jul 3;1(1):67-70. No abstract available.

PMID:
11828400
45.

Chemical synthesis and biological evaluation of cis- and trans-12,13-cyclopropyl and 12,13-cyclobutyl epothilones and related pyridine side chain analogues.

Nicolaou KC, Namoto K, Ritzén A, Ulven T, Shoji M, Li J, D'Amico G, Liotta D, French CT, Wartmann M, Altmann KH, Giannakakou P.

J Am Chem Soc. 2001 Sep 26;123(38):9313-23.

PMID:
11562214
46.

Total synthesis of epothilone B, epothilone D, and cis- and trans-9,10-dehydroepothilone D.

White JD, Carter RG, Sundermann KF, Wartmann M.

J Am Chem Soc. 2001 Jun 13;123(23):5407-13. Erratum in: J Am Chem Soc. 2003 M ar 12;125(10):3190..

PMID:
11389619
47.

Catalytic antibody route to the naturally occurring epothilones: total synthesis of epothilones A-F.

Sinha SC, Sun J, Miller GP, Wartmann M, Lerner RA.

Chemistry. 2001 Apr 17;7(8):1691-702.

PMID:
11349910
48.

Synthesis and biological evaluation of highly potent analogues of epothilones B and D.

Altmann KH, Bold G, Caravatti G, Flörsheimer A, Guagnano V, Wartmann M.

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2765-8.

PMID:
11133086
49.

Chemical synthesis and biological properties of pyridine epothilones.

Nicolaou KC, Scarpelli R, Bollbuck B, Werschkun B, Pereira MM, Wartmann M, Altmann KH, Zaharevitz D, Gussio R, Giannakakou P.

Chem Biol. 2000 Aug;7(8):593-9.

50.

Epothilones and related structures--a new class of microtubule inhibitors with potent in vivo antitumor activity.

Altmann KH, Wartmann M, O'Reilly T.

Biochim Biophys Acta. 2000 May 17;1470(3):M79-91. Review. No abstract available.

PMID:
10799747

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