Waring, Mike - Newcastle University

个人简介

Qualifications BSc(Hons), First Class, in Chemistry 1996 (University of Manchester) PhD in Organic Chemistry 1999 (University of Manchester) with Prof. T. J. Donohoe Previous Positions April 2011 – August 2015: Principal Scientist in Medicinal Chemistry at AstraZeneca, Alderley Park, UK. July 2001 – March 2011: Team Leader in Medicinal Chemistry at AstraZeneca, Alderley Park, UK January 2000 - July 2001: Post-doctoral researcher in the group of Prof. P. D. Magnus, University of Texas at Austin, USA.

近期论文

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Hothersall JD, Guo D, Sarda S, Sheppard RJ, Chen H, Keur W, Waring MJ, IJzerman AP, Hill SJ, Dale IL, Rawlins PB. Structure-activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics. Molecular Pharmacology 2017, 91(1), 25-38. England RM, Hare JI, Barnes J, Wilson J, Smith A, Strittmatter N, Kemmitt PD, Waring MJ, Barry ST, Alexander C, Ashford MB. Tumour regression and improved gastrointestinal tolerability from controlled release of SN-38 from novel polyoxazoline-modified dendrimers. Journal of Controlled Release 2017, 247, 73-85. Rhyasen GW, Hattersley M, Yao Y, Dulak A, Wang W, Petteruti P, Dale I, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh T, Rabow AA, Dry J, Reimer C, Lyne P, Mills GB, Fawell S, Waring MJ, Zinda M, Clark E, Chen H. AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies. Molecular Cancer Therapeutics 2016, 15(11), 2563-2574. England RM, Hare JI, Kemmitt PD, Treacher K, Waring MJ, Barry ST, Alexander C, Ashford M. Enhanced cytocompatibility and functional group content of poly(L-lysine) dendrimers by grafting with poly(oxazolines). Polymer Chemistry 2016, 7(28), 4609-4617. Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Optimisation of a series of bivalent triazolopyridazine based bromodomain and extraterminal inhibitors: the discovery of (3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153). Journal of Medicinal Chemistry 2016, 59(17), 7801-7817. Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale E, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Mendez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y. Potent and selective bivalent inhibitors of BET bromodomains. Nature Chemical Biology 2016, 12, 1097-1104. Bradbury RH, Rabow AA, Waring MJ, McCabe JF, Glossop SC, Mahmood A, Cotter ZA. Preparation of triazolopyridazine derivatives for use as antiproliferative agents. 04/02/2016. Waring MJ, Bennett SNL, Campbell L, Hallam S, Martin NG, Tickner C. A safe and scalable synthesis of 2-hydroxy-3-alkoxypropionates by epoxide ring opening. Tetrahedron Letters 2015, 56(34), 4904-4907. Waring MJ, Arrowsmith J, Leach AR, Leeson PD, Mandrell S, Owen RM, Pairaudeau G, Pennie W, Pickett SD, Wang J, Wallace O, Weir A. An analysis of the attrition of drug candidates from four major pharmaceutical companies. Nature Reviews Drug Discovery 2015, 14, 475-486. Waring MJ, Baker DJ, Bennett SNL, Dossetter AG, Fenwick M, Garcia R, Georgsson J, Groombridge SD, Loxham S, MacFaul PA, Maskill KG, Morgan D, Morrell J, Pointon H, Robb GR, Smith DM, Stokes S, Wilkinson G. Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40. MedChemComm 2015, (6), 1024-1029. Raubo P, Andrews DM, McKelvie JC, Robb GR, Smith JM, Swarbirck ME, Waring MJ. Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα). Bioorganic & Medicinal Chemistry Letters 2015, 25(16), 3189-3193. Gill DM, McLay N, Waring MJ, Wilkinson CT, Sweeney JB. An Improved Method for Difluorocyclopropanation of Alkenes. Synlett 2014, 25(12), 1756-1756. Finlay MRV, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DAE, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. Journal of Medicinal Chemistry 2014, 57(20), 8249-8267. Waring MJ, Andrews DM, Faulder PF, Flemington V, McKelvie JC, Maman S, Preston M, Raubo P, Robb GR, Roberts K, Rowlinson R, Smith JM, Swarbrick ME, Treines I, Winter JG, Wood RJ. Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β- inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation. Chemical Communications 2014, 50(40), 5388-5390. Cumming JG, Finlay MRV, Giordanetto F, Hemmerling M, Lister T, Sanganee H, Waring MJ. The challenges of increasing drug discovery productivity. Future Medicinal Chemistry 2014, 6(5), 515-527. Robb GR, McKerrecher D, Newcombe NJ, Waring MJ. A chemistry Wiki to facilitate and enhance chemical design in drug discovery. Drug Discovery Today 2013, 18(3-4), 141-147. Plowright AT, Barton P, Bennett S, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RDM, Ertan A, MorentinGutierrez P, Kemmitt PD, Leach AG, Svensson PH, Turnbull AV, Waring MJ. Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1. Med. Chem. Commun 2013, 4, 151. Waring MJ, Bennett SNL, Campbell L, Davies RDM, Gerhardt S, Hargreaves D, Martin NG, Robb GR, Wilkinson G. Matched triplicate design sets in the optimisation of glucokinase activators – maximising medicinal chemistry information content. Med. Chem. Commun 2013, 4, 657. Waring MJ, Birch AM, Birtles S, Buckett LK, Butlin RJ, Campbell L, MorentinGutierrez P, Kemmitt P, Leach AG, MacFaul P, ODonnell C, Turnbull AV. Optimisation of biphenylacetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353. Med. Chem. Commun 2013, 4, 159. Waring MJ, Bennett SNL, Campbell L, Davies RDM, Hargreaves D, MacFaul P, Martin NG, Ogg D, Robb GR, Wilkinson G, Wood JM. Optimising pharmacokinetics of glucokinase activators with matched triplicate design sets – the discovery of AZD3651 and AZD9485. Med. Chem. Commun 2013, 4, 663. McKerrecher D, Waring MJ. Property based design in the optimisation of glucokinase activators: from hit to clinic. Progr. Med. Chem 2013, 52, 1. McKerrecher D, Waring MJ. Property-Based Design in the Optimisation of Benzamide Glucokinase Activators: From Hit to Clinic. Progr. Med. Chem 2013, 52, 1. Ward RA, Anderton M, Ashton S, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross D, Debreczeni JE, Eberlein C, Finlay MRV, Grist M, Hill GB, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Structure and reactivity based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). J. Med. Chem 2013, 56, 7025. Waring MJ, Clarke DS, Fenwick MD, Godfrey L, Groombridge S, Johnstone C, McKerrecher D, Pike KG, Rayner J, Robb GR, Wilson I. Property based optimisation of glucokinase activators – the discovery of the Phase IIb candidate AZD1656. Med. Chem. Commun 2012, 3, 1077. Moss T, Addie MS, Nowak T, Waring MJ. Room-temperature palladium-catalyzed coupling of heteroaryl amines with aryl or heteroaryl bromides. Synlett 2012, 23, 285.