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Items: 42

1.

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C.

ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9.

2.

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Caravatti G, Guagnano V, Aichholz R, Blanz J, Blasco F, Wipfli P, Fritsch C, Maira SM, Schnell C, Seiler FH.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4729-4734. doi: 10.1016/j.bmcl.2016.08.041. Epub 2016 Aug 17.

PMID:
27575470
3.

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C.

ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11.

4.

Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Imbach-Weese P, Gerspacher M, Caravatti G, Furet P, Zoller T, Fritsch C, Haasen D, Trappe J, Guthy DA, Arz D, Wirth J.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3569-74. doi: 10.1016/j.bmcl.2015.06.078. Epub 2015 Jun 27.

PMID:
26206504
5.

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Gerspacher M, Imbach-Weese P, Mah R, Caravatti G, Furet P, Fritsch C, Schnell C, Blanz J, Blasco F, Desrayaud S, Guthy DA, Knapp M, Arz D, Wirth J, Roehn-Carnemolla E, Luu VH.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3575-81. doi: 10.1016/j.bmcl.2015.06.067. Epub 2015 Jun 26.

PMID:
26199119
6.

Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

Fritsch C, Huang A, Chatenay-Rivauday C, Schnell C, Reddy A, Liu M, Kauffmann A, Guthy D, Erdmann D, De Pover A, Furet P, Gao H, Ferretti S, Wang Y, Trappe J, Brachmann SM, Maira SM, Wilson C, Boehm M, Garcia-Echeverria C, Chene P, Wiesmann M, Cozens R, Lehar J, Schlegel R, Caravatti G, Hofmann F, Sellers WR.

Mol Cancer Ther. 2014 May;13(5):1117-29. doi: 10.1158/1535-7163.MCT-13-0865. Epub 2014 Mar 7.

7.

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.

PMID:
23726034
8.

Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison.

Weisberg E, Roesel J, Furet P, Bold G, Imbach P, Flörsheimer A, Caravatti G, Jiang J, Manley P, Ray A, Griffin JD.

Genes Cancer. 2010 Oct;1(10):1021-32. doi: 10.1177/1947601910396505.

9.

COL1A2 gene deletion polymorphism in an Italian and an Ivorian populations.

Santovito A, Burgarello C, Cervella P, Caravatti G, Ouattara M, Salvarani B, Delpero M.

Genetika. 2009 Jul;45(7):977-81.

PMID:
19705750
10.

Erythrocyte polymorphisms in five ethnic groups of Northern Côte d'Ivoire.

Santovito A, Burgarello C, Cervella P, Ouattara M, Caravatti GA, Salvarani B, Delpero M.

Int J Immunogenet. 2009 Jun;36(3):189-91. doi: 10.1111/j.1744-313X.2009.00842.x.

PMID:
19490215
11.

ACE and LRPAP1 insertion-deletion polymorphisms in a northern Ivory Coast population.

Santovito A, Burgarello C, Caravatti GA, Ouattará M, Cervella P, Pisano G, Salvarani B, Delpero M.

Hum Biol. 2007 Dec;79(6):699-706. Erratum in: Hum Biol. 2008 Apr;80(2):199. Bulgarello, C [corrected to Burgarello, C].

PMID:
18494379
12.

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Furet P, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

PMID:
18248988
13.

Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models.

Oehler-Jänne C, Jochum W, Riesterer O, Broggini-Tenzer A, Caravatti G, Vuong V, Pruschy M.

Mol Cancer Ther. 2007 Sep;6(9):2496-504.

14.

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.

15.

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
16.

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.

17.

Protein kinases as targets for anticancer agents: from inhibitors to useful drugs.

Fabbro D, Ruetz S, Buchdunger E, Cowan-Jacob SW, Fendrich G, Liebetanz J, Mestan J, O'Reilly T, Traxler P, Chaudhuri B, Fretz H, Zimmermann J, Meyer T, Caravatti G, Furet P, Manley PW.

Pharmacol Ther. 2002 Feb-Mar;93(2-3):79-98. Review.

PMID:
12191602
18.

Tyrosine kinase inhibitors: from rational design to clinical trials.

Traxler P, Bold G, Buchdunger E, Caravatti G, Furet P, Manley P, O'Reilly T, Wood J, Zimmermann J.

Med Res Rev. 2001 Nov;21(6):499-512. Review.

PMID:
11607931
19.

Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne.

Schoepfer J, Gay B, End N, Muller E, Scheffel G, Caravatti G, Furet P.

Bioorg Med Chem Lett. 2001 May 7;11(9):1201-3.

PMID:
11354377
20.

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
21.

Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 2.

Walker CV, Caravatti G, Denholm AA, Egerton J, Faessler A, Furet P, García-Echeverría C, Gay B, Irving E, Jones K, Lambert A, Press NJ, Woods J.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2343-6.

PMID:
11055352
22.

Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1.

Furet P, Caravatti G, Denholm AA, Faessler A, Fretz H, García-Echeverría C, Gay B, Irving E, Press NJ, Rahuel J, Schoepfer J, Walker CV.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2337-41.

PMID:
11055351
23.

Selective GRB2 SH2 inhibitors as anti-Ras therapy.

Gay B, Suarez S, Caravatti G, Furet P, Meyer T, Schoepfer J.

Int J Cancer. 1999 Oct 8;83(2):235-41.

24.

Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.

Caravatti G, Rahuel J, Gay B, Furet P.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1973-8.

PMID:
10450965
25.

Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility.

Gay B, Suarez S, Weber C, Rahuel J, Fabbro D, Furet P, Caravatti G, Schoepfer J.

J Biol Chem. 1999 Aug 13;274(33):23311-5.

26.

Author errata.

Meyer T, Regenass U, Fabbro D, Alteri E, Rösel J, Müller M, Caravatti G, Matter A.

Int J Cancer. 1999 May 17;81(4):669. No abstract available.

27.

Highly potent inhibitors of the Grb2-SH2 domain.

Schoepfer J, Fretz H, Gay B, Furet P, García-Echeverría C, End N, Caravatti G.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):221-6.

PMID:
10021933
28.

Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain.

Schoepfer J, Gay B, Caravatti G, Garcia-Echeverria C, Fretz H, Rahuel J, Furet P.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2865-70.

PMID:
9873638
29.

Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.

Furet P, Gay B, Caravatti G, García-Echeverría C, Rahuel J, Schoepfer J, Fretz H.

J Med Chem. 1998 Aug 27;41(18):3442-9.

PMID:
9719597
30.

Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands.

Rahuel J, García-Echeverría C, Furet P, Strauss A, Caravatti G, Fretz H, Schoepfer J, Gay B.

J Mol Biol. 1998 Jun 19;279(4):1013-22.

PMID:
9642078
31.

Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.

García-Echeverría C, Furet P, Gay B, Fretz H, Rahuel J, Schoepfer J, Caravatti G.

J Med Chem. 1998 May 21;41(11):1741-4. No abstract available.

PMID:
9599224
32.

Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.

Furet P, Gay B, García-Echeverría C, Rahuel J, Fretz H, Schoepfer J, Caravatti G.

J Med Chem. 1997 Oct 24;40(22):3551-6.

PMID:
9357522
33.

Dual specificity of Src homology 2 domains for phosphotyrosine peptide ligands.

Gay B, Furet P, García-Echeverría C, Rahuel J, Chène P, Fretz H, Schoepfer J, Caravatti G.

Biochemistry. 1997 May 13;36(19):5712-8.

PMID:
9153411
34.

Phenylamino-pyrimidine (PAP) derivatives: a new class of potent and selective inhibitors of protein kinase C (PKC).

Zimmermann J, Caravatti G, Mett H, Meyer T, Müller M, Lydon NB, Fabbro D.

Arch Pharm (Weinheim). 1996 Jul;329(7):371-6.

PMID:
8764886
35.

Structural basis for specificity of Grb2-SH2 revealed by a novel ligand binding mode.

Rahuel J, Gay B, Erdmann D, Strauss A, Garcia-Echeverría C, Furet P, Caravatti G, Fretz H, Schoepfer J, Grütter MG.

Nat Struct Biol. 1996 Jul;3(7):586-9. No abstract available.

PMID:
8673601
36.

In vitro trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors.

Brun R, Bühler Y, Sandmeier U, Kaminsky R, Bacchi CJ, Rattendi D, Lane S, Croft SL, Snowdon D, Yardley V, Caravatti G, Frei J, Stanek J, Mett H.

Antimicrob Agents Chemother. 1996 Jun;40(6):1442-7.

37.

Modelling study of protein kinase inhibitors: binding mode of staurosporine and origin of the selectivity of CGP 52411.

Furet P, Caravatti G, Lydon N, Priestle JP, Sowadski JM, Trinks U, Traxler P.

J Comput Aided Mol Des. 1995 Dec;9(6):465-72.

PMID:
8789188
38.

4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase.

Stanek J, Caravatti G, Frei J, Furet P, Mett H, Schneider P, Regenass U.

J Med Chem. 1993 Jul 23;36(15):2168-71.

PMID:
8340919
39.

Differential inhibition of human secretory and cytosolic phospholipase A2.

Märki F, Breitenstein W, Beriger E, Bernasconi R, Caravatti G, Francis JE, Paioni R, Wehrli HU, Wiederkehr R.

Agents Actions. 1993 Mar;38(3-4):202-11.

PMID:
8213347
40.

S-adenosylmethionine decarboxylase inhibitors: new aryl and heteroaryl analogues of methylglyoxal bis(guanylhydrazone).

Stanek J, Caravatti G, Capraro HG, Furet P, Mett H, Schneider P, Regenass U.

J Med Chem. 1993 Jan 8;36(1):46-54.

PMID:
8421290
41.

New S-adenosylmethionine decarboxylase inhibitors with potent antitumor activity.

Regenass U, Caravatti G, Mett H, Stanek J, Schneider P, Müller M, Matter A, Vertino P, Porter CW.

Cancer Res. 1992 Sep 1;52(17):4712-8.

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