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Robert D M Davies

Explore the profile of Robert D M Davies including associated specialties, affiliations and a list of published articles. Areas
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Articles 12
Citations 106
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Recent Articles
1.
Scott J, Bailey A, Buttar D, Carbajo R, Curwen J, Davey P, et al.
J Med Chem . 2019 Jan; 62(3):1593-1608. PMID: 30640465
Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our...
2.
Paterson I, Davies R, Marquez R
Angew Chem Int Ed Engl . 2018 May; 40(3):603-607. PMID: 29712021
Following macrolactonization, a Sonogashira coupling leads efficiently from 1 and 2 to the aglycon of the structurally unique cytotoxic macrolide callipeltoside A, isolated in tiny quantities from the lithistid sponge...
3.
Scott J, Degorce S, Anjum R, Culshaw J, Davies R, Davies N, et al.
J Med Chem . 2017 Nov; 60(24):10071-10091. PMID: 29172502
Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize...
4.
Scott J, Bailey A, Davies R, Degorce S, MacFaul P, Gingell H, et al.
ACS Med Chem Lett . 2016 Jan; 7(1):94-9. PMID: 26819673
A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile. Optimization around the core, alkyl side chain, and pendant aryl ring resulted in compounds with subnanomolar...
5.
Wlochal J, Davies R, Burton J
Org Lett . 2014 Jul; 16(16):4094-7. PMID: 25068498
A collection of novel, pharmaceutically relevant cubane-containing molecules has been prepared from the commercially available cubane-1,4-dimethylester. A range of synthetic methods have been applied to prepare these cubane building blocks...
6.
McCoull W, Barton P, Brown A, Bowker S, Cameron J, Clarke D, et al.
J Med Chem . 2014 Jun; 57(14):6128-40. PMID: 24967667
Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by...
7.
Czyzewski M, Sellars J, Guliashvili T, Tibbelin J, Johnstone L, Bower J, et al.
Chem Commun (Camb) . 2014 Feb; 50(22):2919-21. PMID: 24496122
The synthesis of silaheterocycles through the first examples of an intramolecular silene Diels-Alder reaction is described.
8.
Barlind J, Bauer U, Birch A, Birtles S, Buckett L, Butlin R, et al.
J Med Chem . 2012 Nov; 55(23):10610-29. PMID: 23116186
A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low...
9.
Nazef N, Davies R, Greaney M
Org Lett . 2012 Jul; 14(14):3720-3. PMID: 22770228
A formal synthesis of merrilactone A has been completed using a domino 1,4-addition-aldol process as the key step. Both iodo- and cyano-1,4-addition-aldol cyclizations were productive in forming the highly hindered...
10.
McCoull W, Addie M, Birch A, Birtles S, Buckett L, Butlin R, et al.
Bioorg Med Chem Lett . 2012 May; 22(12):3873-8. PMID: 22608962
A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid...