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Items: 13

1.

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
2.

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.

3.

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
4.

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
5.

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
6.

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.

7.

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
8.

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
9.

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.

10.

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
11.

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
12.

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.

13.

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

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