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Dr Mathew Leese: Publications, Patents & Conferences - 1997-2012

Publications
Steroidomimetic tetrahydroisoquinolines for the design of new microtubule disruptors. Leese, M. P.; Jourdan, F.; Dohle, W.; Kimberley, M. R.; Thomas, M. P.; Bai, R.; Hamel, E.; Ferrandis, E.; Potter, B. V. L. ACS MedChemLett 2012, 3, 5-9.
Structure-Activity Relationships of C-17-substituted estratriene-3-O-sulfamates as anticancer Jourdan, F.; Leese, M. P.; Dohle, W.; Ferrandis, E.; Newman, S. P.; Chander, S.; Purohit, A.; Potter, B. V. L. J. Med. Chem. 2011, 54, 4863-4879.
Discovery of chimeric microtubule disruptors. Leese, M.P.; Jourdan, F.; Kimberley, M.R.; Cozier, G.E.; Thiyagarajan, N.; Stengel, C.; Regis-Lydi, S.;, Foster, P.A.; Newman, S.P.; Acharya, K.R.; Ferrandis, E.; Purohit, A.; Reed, M.J.; Potter, B.V.L. Chem Commun 2010, 46, 2907. Cover article 7th May 2010, selected for RSC highlights in Chemical Biology. Structures of human carbonic anhydrase II/inhibitor complexes reveal a second binding site for steroidal and non-steroidal inhibitors. Cozier, G.; Leese, M.P.; Lloyd, M.; Baker, M.; Thiyagarajan, N.; Acharya, K.R.; Potter, B.V.L. Biochemistry 2010, 49, 3464-3476. Synthesis, Antitubulin and Antiproliferative SAR of Analogues of 2-Methoxyestradiol-3,17- O,O-bissulfamate. Jourdan, F.; Leese, M.P; Dohle, W; Hamel, E.; Ferrandis, E.; Newman, S.P.; Purohit A.; Reed, M.J.; Potter, B.V.L. J Med Chem 2010, 53, 2942-51. -tubulin expression and in vitro resistance to microtubule targeting agents Stengel, C.; Newman, S.P.; Leese, M.P.; Potter, M.P.; Reed, M.J.; Purohit, A. Br J Cancer 2010, 102, 316-324. STX140 and STX641 Cause Apoptosis via the Intrinsic Mitochondrial Pathway and Down- regulate Survivin and XIAP Expression in Ovarian and Prostate Cancer Cells. Foster, P. A.; Ho, Y. T.; Newman, S. P.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A. Anticancer Research 2009, 29
BCRP expression does not result in resistance to STX140 in vivo, despite the increased expression of BCRP in A2780 cells in vitro after long-term STX140 exposure. Day, J. M.; Foster, P. A.; Tutil , H. J.; Newman, S. P.; Ho, Y. T.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A. Br J A new micronized formulation of 2-methoxyestradiolbis-sulfamate (STX140) is therapeutical y potent against breast cancer. Foster, P. A.; Newman, S. P.; Leese, M. P.; Bernetiere, S.; Diolez, C.; Camara, J.; Hacher, B.; Baronnet, M. M.; Ali, T.; Potter, B. V. L.; Reed, M. J.; Purohit, A. Anticancer A comparison of two orally bioavailable anti-cancer agents, IRC-110160 and STX140. Foster, P. A.; Stengel, C.; Ali, T.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A.; Newman, S. P. Anticancer Res 2008, 28, 1483-1491. The in vivo properties of STX243: a potent angiogenesis inhibitor in breast cancer. Parsons, M. F. C.; Foster, P. A.; Chander, S. K.; Jhal i, R.; Newman, S. P.; Leese, M. P.; Potter, B. V. L.; Purohit, A.; Reed, M. J. Br J Cancer 2008, 99, 1433-1441. 2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer. Tagg, S. L. C.; Foster, P. A.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A.; Newman, S. P. Br J Cancer 2008, 99, 1842-1848. Effects of C-17 heterocyclic substituents on the anticancer activity of 2-ethylestra-1,3,5(10)- triene-3-O-sulfamates: synthesis, in vitro evaluation and computational modeling. Jourdan, F.; Bubert, C.; Leese, M. P.; Smith, A.; Ferrandis, E.; Regis-Lydi, S.; Newman, S. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. Org Biomol Chem 2008, 6, 4108-4119. 2-MeOE2bisMATE and 2-EtE2bisMATE induce cel cycle arrest and apoptosis in breast cancer xenografts as shown by a novel ex vivo technique. Foster, P. A.; Ho, Y. T.; Raobaikady, B.; Newman, S. P.; Kasprzyk, P. G.; Leese, M. P.; Potter, B. V. L.; Reed M. J.; Purohit, A. Breast Cancer STX140, is efficacious in vitro and in vivo in taxane resistant breast carcinoma cells. Newman, S. P.; Foster, P. A.; Stengel, C.; Day, J.M.; Ho, Y.T.; Judde, J.-G.; Lassal e, M.; Prevost, G.; Leese, M. P.; Potter, B. V. L.; Reed M. J.;Purohit, A. Clin Cancer Res 2008, 14, 597-606. Structure-activity relationships of C-17 cyanated estratrienes as anti-cancer agents. Leese M. P.; Jourdan F. L.; Gaukroger, K.; Mahon, M. F.; Newman, S. P.; Foster, P. A.; Stengel, C.; Regis-Lydi, S.; Ferrandis, E.; Di Fiore, A.; De Simone, G.; Supuran, C. T.; Purohit, A.; Reed M. J.; Potter, B. V. L. The therapeutic potential of a series of oral y bioavailable antiangiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers. Newman, S. P.; Foster, P. A.; Ho, Y. T.; Day, J. M.; Raobaikady, B.; Kasprzyk, P. G.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A. Br J Cancer 2007, 97, 1673-1682. 3,17-Disubstituted 2-Alkylestra-1,3,5(10)-trien-3-ol derivatives: Synthesis, in vitro and in vivo anticancer activity. Bubert, C.; Leese, M. P.; Mahon, M. F.; Ferrandis, E.; Regis-Lydi, S.; Kasprzyk, P. G.; Newman, S. P.; Ho, Y. T.; Purohit, A.; Reed, M. J.; Potter, B. V. L. J Med Chem 2007, 50, 4431- In vivo inhibition of angiogenesis by sulphamoylated derivatives of 2-methoxyoestradiol. Chander, S. K.; Foster, P. A.; Leese, M. P.; Newman, S. P.; Potter, B. V. L.; Purohit, A.; Reed, M. J. 2-Substituted estradiol bis-sulfamates, multitargeted antitumor agents: Synthesis, in vitro SAR, protein crystallography, and in vivo activity. Leese, M. P.; Leblond, B.; Smith, A.; Newman, S. P.; Di Fiore, A.; De Simone, G.; Supuran, C. T.; Purohit, A.; Reed, M. J.; Potter, B. V. L. J Med Chem -hydroxysteroid dehydrogenases in modulating the activity of 2- methoxyestradiol in breast cancer cells. Newman, S. P.; Ireson, C. R.; Tutil , H. J.; Day, J. M.; Parsons, M. F. C.; Leese, M. P.; Potter, B. V. L.; Reed, M. J.; Purohit, A. Cancer Res 2006, 66, 324- Inhibition of MDA-MB-231 cell cycle progression and cell proliferation by C-2-substituted oestradiol mono- and bis-3-O-sulphamates.Raobaikady, B.; Reed, M. J.; Leese, M. P.; Potter, B. V. L.; Purohit, A. Int J Cancer 2005, 117, 150-159. A-Ring-substituted estrogen-3-O-sulfamates: Potent multitargeted anticancer agents. Leese, M. P.; Hejaz, H. A. M.; Mahon, M. F.; Newman, S. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. J Med Regulation of aromatase activity by cytokines, PGE2 and 2-methoxyoestrone-3-O-sulphamate in fibroblasts derived from normal and malignant breast tissues. Purohit, A.; Ghilchik, M. W.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2005, 94, 167-172. The effects of 2-methoxyoestrogen sulpharnates on the in vitro and in vivo proliferation of breast cancer cel s. Utsumi, T.; Leese, M. P.; Chander, S. K.; Gaukroger, K.; Purohit, A.; Newman, S. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2005, 94, 219-227. Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates. Leese, M. P.; Leblond, B.; Newman, S. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. J Steroid Biochem Mol 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents. Leese, M. P.; Newman, S. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. Bioorg Med Chem Lett 2-MeOE2bisMATE induces caspase-dependent apoptosis in CAL51 breast cancer cells and overcomes resistance to TRAIL via cooperative activation of caspases. Wood, L.; Leese, M. P.; Mouzakiti, A.; Purohit, A.; Potter, B. V. L.; Reed, M. J.; Packham, G. Apoptosis 2004, 9, 323-332. 2-Difluoromethyloestrone 3-O-sulphamate, a highly potent steroid sulphatase inhibitor. Reed, J. E.; Woo, L. W. L.; Robinson, J. J.; Leblond, B.; Leese, M. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. Biochem Biophys Res Comm 2004, 317, 169-175. Inhibition of in vitro angiogenesis by 2-methoxy- and 2-ethyl-estrogen sulfamates. Newman, S. P.; Leese, M. P.; Purohit, A.; James, D. R. C.; Rennie, C. E.; Potter, B. V. L.; Reed, M. J. Int J Pharmacokinetics and efficacy of 2-methoxyoestradiol and 2-methoxyoestradiol-bis- sulphamate in vivo in rodents. Ireson, C. R.; Chander, S. K.; Purohit, A.; Perera, S.; Newman, S. P.; Parish, D.; Leese, M. P.; Smith, A. C.; Potter, B. V. L.; Reed, M. J. Br J Cancer 2004, 90, 932-937. Steroid sulphatase inhibitors for breast cancer therapy. Purohit, A.; Woo, L. W. L.; Chander, S. K.; Newman, S. P.; Ireson, C.; Ho, Y.; Grasso, A.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2003, 86, 423-432. The effects of 2-methoxy oestrogens and their sulphamoylated derivatives in conjunction with TNF-alpha on endothelial and fibroblast cel growth, morphology and apoptosis.Ho, Y. T.; Newman, S. P.; Purohit, A.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2003, 86, 189- Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates. Ho, Y. T.; Purohit, A.; Vicker, N.; Newman, S. P.; Robinson, J. J.; Leese, M. P.; Ganeshapil ai, D.; Woo, L. W. L.; Potter, B. V. L.; Reed, M. J. Biochem Biophys Res Comm 2003, 305, 909-914. Growth inhibition of multi-drug-resistant breast cancer cells by 2-methoxyoestradiol-bis- sulphamate and 2-ethyloestradiol-bis-sulphamate.Suzuki, R. N.; Newman, S. P.; Purohit, A.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2003, 84, 269-278. The effects of 2-substituted oestrogen sulphamates on the growth of prostate and ovarian cancer cells. Day, J. M.; Newman, S. P.; Comninos, A.; Solomon, C.; Purohit, A.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2003, 84, 317-325. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2- methoxyoestradiol-bis-sulphamate. Raobaikady, B.; Purohit, A.; Chander, S. K.; Woo, L. W. L.; Leese, M. P.; Potter, B. V. L.; Reed, M. J. J Steroid Biochem Mol Biol 2003, 84, 351-358. Inhibition of superoxide dismutase by 2-methoxyoestradiol analogues and oestrogen derivatives: structure-activity relationships. Wood, L.; Leese, M. P.; Leblond, B.; Woo, L. W. L.; Ganeshapil ai, D.; Purohit, A.; Reed, M. J.; Potter, B. V. L.; Packham, G. Anti-Cancer Drug Des 2001, A survey of suitable protecting groups for the synthesis of hydroxylamines by Mitsunobu reactions. Knight, D. W.; Leese, M. P. Tetrahedron Lett 2001, 42, 2593-2595. The synthesis of N-hydroxyisoindolines by reverse-Cope chemistry. Knight, D. W.; Leese, M. P.; De Kimpe, N. Tetrahedron Lett 2001, 42, 2597-2600. Palladium catalysed coupling reactions using guanidinium phosphine complexes on glass beads. Leese, M. P.; Wil iams, J. M. J. Synlett 1999, 1645-1647. Transition metal catalysed reactions using glass bead technology.Anson, M. S.; Leese, M. P.; Tonks, L.; Wil iams, J. M. J. J Chem Soc Dalton Trans 1998, 3529-3538. Optimisation of palladium-based supported liquid-phase catalysts in the Heck reaction.Mirza, A. R.; Anson, M. S.; Hel gardt, K.; Leese, M. P.; Thompson, D. F.; Tonks, L.; Wil iams, J. M. J. Org Al ene formation by the reaction of olefins with propargyl silyl ethers mediated by a zirconocene complex. Takahashi, T.; Hara, R.; Huo, S. Q.; Ura, Y.; Leese, M. P.; Suzuki, N. Tetrahedron Lett 1997, 38, 8723-8726. A new, stereoselective, approach to pyrrolidine-N-oxides by sequential condensation of sulfones with nitrones and reverse-Cope elimination. Wheildon, A. R.; Knight, D. W.; Leese, M. P. Tetrahedron Lett 1997, 38, 8553-8556.
WO 2008/117061: Compound
US 20070225256: 2-Substituted estrogen sulphamates for inhibition of steroid sulphatase
US 20060094696: Oestrogen derivatives for inhibition of steroid sulphatase
US 7,119,081: Oestrogen-17-sulphamates as inhibitors of steroid sulphatase
US 7,067,503: 17-aryl linker derivatised estrogen 3-sulphamates as inhibitors of steroid sulphatase
Conference Presentations
February 2011: Comprehensive Approach to Cancer and Infectious Disease, Okayama, Japan (Invited lecture). November 2010: AACR NCI EORTC Molecular Targets and Cancer Therapeutics Meeting, Berlin, Germany (Poster). April 2009: AACR Annual Meeting, Denver CO (Poster). April 2008: AACR Annual Meeting, San Diego, CA (Oral). November 2007: AACR NCI EORTC Molecular Targets and Cancer Therapeutics Meeting, San Francisco, CA (Poster). September 2006: XVth European Conference of the GP2A, Bath, UK (Oral). April 2006: AACR Annual Meeting, Washington DC (Poster). November 2005: AACR NCI EORTC Molecular Targets and Cancer Therapeutics Meeting, Philadelphia, PA (Poster). September 2004: AACR NCI EORTC Molecular Targets and Cancer Therapeutics Meeting, Geneva, January 2002: Novabiochem Parallel Synthesis Meeting, Basel, Switzerland. August 2000: ACS Fal National Meeting, Washington, DC (Poster). June 1997: RSC Heterocyclic Group Symposium, Keele, UK (Oral). April 1997: ACS Spring National Meeting, San Francisco, CA (Poster).

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