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Items: 1 to 50 of 107

1.

Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.

Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X.

J Med Chem. 2020 Feb 13. doi: 10.1021/acs.jmedchem.9b01720. [Epub ahead of print]

PMID:
32023060
2.

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.

Goldberg FW, Finlay MRV, Ting AKT, Beattie D, Lamont GM, Fallan C, Wrigley GL, Schimpl M, Howard MR, Williamson B, Vazquez-Chantada M, Barratt DG, Davies BR, Cadogan EB, Ramos-Montoya A, Dean E.

J Med Chem. 2020 Jan 15. doi: 10.1021/acs.jmedchem.9b01684. [Epub ahead of print]

PMID:
31851518
3.

AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity.

Fok JHL, Ramos-Montoya A, Vazquez-Chantada M, Wijnhoven PWG, Follia V, James N, Farrington PM, Karmokar A, Willis SE, Cairns J, Nikkilä J, Beattie D, Lamont GM, Finlay MRV, Wilson J, Smith A, O'Connor LO, Ling S, Fawell SE, O'Connor MJ, Hollingsworth SJ, Dean E, Goldberg FW, Davies BR, Cadogan EB.

Nat Commun. 2019 Nov 7;10(1):5065. doi: 10.1038/s41467-019-12836-9.

4.

Relationship between unintentional canal overfilling and the long-term outcome of primary root canal treatments and nonsurgical retreatments: a retrospective radiographic assessment.

Goldberg F, Cantarini C, Alfie D, Macchi RL, Arias A.

Int Endod J. 2020 Jan;53(1):19-26. doi: 10.1111/iej.13209. Epub 2019 Sep 30.

PMID:
31454090
5.

Controlling the crystalline structure of imine-linked 3D covalent organic frameworks.

Fischbach DM, Rhoades G, Espy C, Goldberg F, Smith BJ.

Chem Commun (Camb). 2019 Mar 21;55(25):3594-3597. doi: 10.1039/c8cc09571j.

PMID:
30839025
6.

Evolution of Small Molecule Kinase Drugs.

Lightfoot HL, Goldberg FW, Sedelmeier J.

ACS Med Chem Lett. 2018 Dec 18;10(2):153-160. doi: 10.1021/acsmedchemlett.8b00445. eCollection 2019 Feb 14.

7.

Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors.

Spender LC, Ferguson GJ, Hughes GD, Davies BR, Goldberg FW, Herrera B, Taylor RG, Strathearn LS, Sansom OJ, Barry ST, Inman GJ.

Mol Pharmacol. 2019 Feb;95(2):222-234. doi: 10.1124/mol.118.112946. Epub 2018 Nov 20.

PMID:
30459156
8.

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.

McCoull W, Hennessy EJ, Blades K, Chuaqui C, Dowling JE, Ferguson AD, Goldberg FW, Howe N, Jones CR, Kemmitt PD, Lamont G, Varnes JG, Ward RA, Yang B.

ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. eCollection 2016 Dec 8.

9.

Accuracy of electronic apex locators to detect root canal perforations with inserted metallic posts: an ex vivo study.

Marroquín BB, Fernández CC, Schmidtmann I, Willershausen B, Goldberg F.

Head Face Med. 2014 Dec 23;10:57. doi: 10.1186/s13005-014-0057-2.

10.

Designing novel building blocks is an overlooked strategy to improve compound quality.

Goldberg FW, Kettle JG, Kogej T, Perry MW, Tomkinson NP.

Drug Discov Today. 2015 Jan;20(1):11-7. doi: 10.1016/j.drudis.2014.09.023. Epub 2014 Oct 2. Review.

PMID:
25281855
11.

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.

Goldberg FW, Dossetter AG, Scott JS, Robb GR, Boyd S, Groombridge SD, Kemmitt PD, Sjögren T, Gutierrez PM, deSchoolmeester J, Swales JG, Turnbull AV, Wild MJ.

J Med Chem. 2014 Feb 13;57(3):970-86. doi: 10.1021/jm4016729. Epub 2014 Jan 27.

PMID:
24422550
12.

Rho kinase inhibition drives megakaryocyte polyploidization and proplatelet formation through MYC and NFE2 downregulation.

Avanzi MP, Goldberg F, Davila J, Langhi D, Chiattone C, Mitchell WB.

Br J Haematol. 2014 Mar;164(6):867-76. doi: 10.1111/bjh.12709. Epub 2014 Jan 2.

PMID:
24383889
13.

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

Scott JS, Goldberg FW, Turnbull AV.

J Med Chem. 2014 Jun 12;57(11):4466-86. doi: 10.1021/jm4014746. Epub 2013 Dec 13. Review.

PMID:
24294985
14.

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms.

Harno E, Cottrell EC, Yu A, DeSchoolmeester J, Gutierrez PM, Denn M, Swales JG, Goldberg FW, Bohlooly-Y M, Andersén H, Wild MJ, Turnbull AV, Leighton B, White A.

Endocrinology. 2013 Dec;154(12):4580-93. doi: 10.1210/en.2013-1613. Epub 2013 Oct 29.

15.

Aziridine-based concise synthesis of (±)-alstonerine.

Craig D, Goldberg FW, Pett RW, Tholen NT, White AJ.

Chem Commun (Camb). 2013 Oct 18;49(81):9275-7. doi: 10.1039/c3cc45543b.

PMID:
23999623
16.

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.

Goldberg FW, Leach AG, Scott JS, Snelson WL, Groombridge SD, Donald CS, Bennett SN, Bodin C, Gutierrez PM, Gyte AC.

J Med Chem. 2012 Dec 13;55(23):10652-61. doi: 10.1021/jm3013163. Epub 2012 Nov 28.

PMID:
23153367
17.

Asymmetric synthesis of 2-alkyl-substituted tetrahydroquinolines by an enantioselective aza-Michael reaction.

Taylor LL, Goldberg FW, Hii KK.

Org Biomol Chem. 2012 Jun 14;10(22):4424-32. doi: 10.1039/c2ob25122a. Epub 2012 May 8.

18.

Papillary lesions of the breast: impact of breast pathology subspecialization on core biopsy and excision diagnoses.

Jakate K, De Brot M, Goldberg F, Muradali D, O'Malley FP, Mulligan AM.

Am J Surg Pathol. 2012 Apr;36(4):544-51. doi: 10.1097/PAS.0b013e318243fa00.

PMID:
22314186
19.

Papillary lesions of the breast: MRI, ultrasound, and mammographic appearances.

Eiada R, Chong J, Kulkarni S, Goldberg F, Muradali D.

AJR Am J Roentgenol. 2012 Feb;198(2):264-71. doi: 10.2214/AJR.11.7922. Review.

PMID:
22268167
20.

[Summary of the 6th Conference of postgraduate physicians of the Medical School of the ULB].

Serroukh Y, Baudoux T, Layeux B, Brauner J, Willems N, Lemoine C, Legrand F, Goldberg F, Frenkel C, Lalmand M, Etienne A, Goldberg O.

Rev Med Brux. 2011 Mar-Apr;32(2):102-7. French. No abstract available. Erratum in: Rev Med Brux. 2011 Sep-Oct;32(5):489.

PMID:
21688595
21.

Tax credits for health insurance.

Goldberg FT Jr, Camic S.

J Law Med Ethics. 2009 Fall;37 Suppl 2:71-85. doi: 10.1111/j.1748-720X.2009.00421.x. No abstract available.

PMID:
19754653
22.

Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).

Goldberg FW, Ward RA, Powell SJ, Debreczeni JE, Norman RA, Roberts NJ, Dishington AP, Gingell HJ, Wickson KF, Roberts AL.

J Med Chem. 2009 Dec 10;52(23):7901-5. doi: 10.1021/jm900807w.

PMID:
19736928
23.

The changing landscape of cancer drug discovery: a challenge to the medicinal chemist of tomorrow.

Pors K, Goldberg FW, Leamon CP, Rigby AC, Snyder SA, Falconer RA.

Drug Discov Today. 2009 Nov;14(21-22):1045-50. doi: 10.1016/j.drudis.2009.07.004. Epub 2009 Jul 26. Review.

PMID:
19638319
24.

The evaluation of four electronic apex locators in teeth with simulated horizontal oblique root fractures.

Goldberg F, Frajlich S, Kuttler S, Manzur E, Briseño-Marroquín B.

J Endod. 2008 Dec;34(12):1497-9. doi: 10.1016/j.joen.2008.09.002. Epub 2008 Oct 18.

PMID:
19026881
25.
26.

Influence of instrument size on the accuracy of different apex locators: an in vitro study.

Briseño-Marroquín B, Frajlich S, Goldberg F, Willershausen B.

J Endod. 2008 Jun;34(6):698-702. doi: 10.1016/j.joen.2008.02.019. Epub 2008 Apr 11.

PMID:
18498892
27.

Optimal multiplexed sensing: bounds, conditions and a graph theory link.

Ratner N, Schechner YY, Goldberg F.

Opt Express. 2007 Dec 10;15(25):17072-92.

PMID:
19551000
28.

An expedient formal total synthesis of (-)-diazonamide A via a powerful, stereoselective O-aryl to C-aryl migration to form the C10 quaternary center.

Cheung CM, Goldberg FW, Magnus P, Russell CJ, Turnbull R, Lynch V.

J Am Chem Soc. 2007 Oct 10;129(40):12320-7. Epub 2007 Sep 19.

29.

Outlook: the profit problem in antibiotic R&D.

Nathan C, Goldberg FM.

Nat Rev Drug Discov. 2005 Nov;4(11):887-91. doi: 10.1038/nrd1878. Review.

PMID:
16247440
30.

A mild thermal and acid-catalyzed rearrangement of O-aryl ethers into ortho-hydroxy arenes.

Goldberg FW, Magnus P, Turnbull R.

Org Lett. 2005 Sep 29;7(20):4531-4.

PMID:
16178576
31.

In vitro evaluation of the ability of three apex locators to determine the working length during retreatment.

Goldberg F, Marroquín BB, Frajlich S, Dreyer C.

J Endod. 2005 Sep;31(9):676-8.

PMID:
16123705
32.

Evaluation of the incidence of transportation after placement and removal of calcium hydroxide.

Goldberg F, Alfie D, Roitman M.

J Endod. 2004 Sep;30(9):646-8.

PMID:
15329569
33.

Reinforcing effect of a resin glass ionomer in the restoration of immature roots in vitro.

Goldberg F, Kaplan A, Roitman M, Manfré S, Picca M.

Dent Traumatol. 2002 Apr;18(2):70-2.

PMID:
12184214
34.

Patency file and apical transportation: an in vitro study.

Goldberg F, Massone EJ.

J Endod. 2002 Jul;28(7):510-1.

PMID:
12126377
35.

In vitro measurement accuracy of an electronic apex locator in teeth with simulated apical root resorption.

Goldberg F, De Silvio AC, Manfré S, Nastri N.

J Endod. 2002 Jun;28(6):461-3.

PMID:
12067130
36.

Influence of calcium hydroxide dressing on the obturation of simulated lateral canals.

Goldberg F, Artaza LP, De S.

J Endod. 2002 Feb;28(2):99-101.

PMID:
11833698
37.

Effectiveness of different obturation techniques in the filling of simulated lateral canals.

Goldberg F, Artaza LP, De Silvio A.

J Endod. 2001 May;27(5):362-4.

PMID:
11485258
38.

Comparison of different techniques for obturating experimental internal resorptive cavities.

Goldberg F, Massone EJ, Esmoris M, Alfie D.

Endod Dent Traumatol. 2000 Jun;16(3):116-21.

PMID:
11202867
39.

Nicotinic acetylcholine currents of cultured Kkenyon cells from the mushroom bodies of the honey bee Aapis mellifera.

Goldberg F, Grünewald B, Rosenboom H, Menzel R.

J Physiol. 1999 Feb 1;514 ( Pt 3):759-68.

40.

Radiographic assessment of simulated external root resorption cavities in maxillary incisors.

Goldberg F, De Silvio A, Dreyer C.

Endod Dent Traumatol. 1998 Jun;14(3):133-6.

PMID:
9863423
41.

Comparative study of retreatment of Thermafil and lateral condensation endodontic fillings.

Frajlich SR, Goldberg F, Massone EJ, Cantarini C, Artaza LP.

Int Endod J. 1998 Sep;31(5):354-7.

PMID:
9823139
42.

[Health and violence as perceived by young people, a study of the Parisian region].

Ginot L, Ait-Bouali N, Besse M, Chevallier P, Goldberg F, Buisson J.

Sante Publique. 1997 Dec;9(4):379-96. French.

PMID:
9584560
43.

Comparison of three instruments in the preparation of curved root canals.

Goldberg F, Araujo JA.

Endod Dent Traumatol. 1997 Dec;13(6):265-8.

PMID:
9558507
44.

Mammographic density in women on postmenopausal hormone replacement therapy.

Leung W, Goldberg F, Zee B, Sterns E.

Surgery. 1997 Oct;122(4):669-73; discussion 673-4.

PMID:
9347841
45.

The CD-ROM as a multipurpose clinical and management tool.

Lieberman HJ, Goldberg F, Kaplan G.

Psychiatr Serv. 1997 Aug;48(8):1014-6. No abstract available.

PMID:
9255832
46.

Disintegration of endodontic cements in water.

Kaplan AE, Goldberg F, Artaza LP, de Silvio A, Macchi RL.

J Endod. 1997 Jul;23(7):439-41.

PMID:
9587297
47.

Apical sealing ability of a new glass ionomer root canal sealer.

Goldberg F, Artaza LP, De Silvio A.

J Endod. 1995 Oct;21(10):498-500.

PMID:
8596069
48.

Comparison of the sealing capacity of three endodontic filling techniques.

Goldberg F, Massone EJ, Artaza LP.

J Endod. 1995 Jan;21(1):1-3.

PMID:
7714427
49.

Interval breast cancers in the Screening Mammography Program of British Columbia: analysis and classification.

Burhenne HJ, Burhenne LW, Goldberg F, Hislop TG, Worth AJ, Rebbeck PM, Kan L.

AJR Am J Roentgenol. 1994 May;162(5):1067-71; discussion 1072-5.

PMID:
8165983
50.

Evaluation of the dimensional stability of different thermoplasticized gutta-percha fillings using simulated glass root canals.

Capurro MA, Goldberg F, Balbachan L, Macchi RL.

Endod Dent Traumatol. 1993 Aug;9(4):160-4.

PMID:
8269881

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