Simon Newman

Summary

Affiliation: Imperial College
Country: UK

Publications

  1. ncbi request reprint The role of 17beta-hydroxysteroid dehydrogenases in modulating the activity of 2-methoxyestradiol in breast cancer cells
    Simon P Newman
    Endocrinology and Metabolic Medicine, Faculty of Medicine, Imperial College, St Mary s Hospital, London, United Kingdom
    Cancer Res 66:324-30. 2006
  2. pmc Class III beta-tubulin expression and in vitro resistance to microtubule targeting agents
    C Stengel
    Oncology Drug Discovery and Women s Health Group, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 102:316-24. 2010
  3. pmc 2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer
    S L C Tagg
    Oncology Drug Discovery and Women s Health Group, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 99:1842-8. 2008
  4. ncbi request reprint Eribulin, a simplified ketone analog of the tubulin inhibitor halichondrin B, for the potential treatment of cancer
    Simon Newman
    Endocrinology and Metabolic Medicine, and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, Norfolk Place, London W2 1NY, UK
    Curr Opin Investig Drugs 8:1057-66. 2007
  5. pmc The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers
    S P Newman
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 97:1673-82. 2007
  6. doi request reprint STX140 is efficacious in vitro and in vivo in taxane-resistant breast carcinoma cells
    Simon P Newman
    Endocrinology and Metabolic Medicine, Faculty of Medicine, Imperial College London, St Mary s Hospital, London, UK
    Clin Cancer Res 14:597-606. 2008
  7. ncbi request reprint Growth inhibition of multi-drug-resistant breast cancer cells by 2-methoxyoestradiol-bis-sulphamate and 2-ethyloestradiol-bis-sulphamate
    R N Suzuki
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 84:269-78. 2003
  8. ncbi request reprint The effects of 2-methoxyoestrogen sulphamates on the in vitro and in vivo proliferation of breast cancer cells
    T Utsumi
    Endocrinology and Metabolic Medicine, Imperial College Faculty of Medicine, St Mary s Hospital and Sterix Ltd, London, W2 1NY, UK
    J Steroid Biochem Mol Biol 94:219-27. 2005
  9. pmc The in vivo properties of STX243: a potent angiogenesis inhibitor in breast cancer
    M F C Parsons
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 99:1433-41. 2008
  10. ncbi request reprint Steroid sulfatase: molecular biology, regulation, and inhibition
    M J Reed
    Endocrinology and Metabolic Medicine, Imperial College, St Mary s Hospital, London W2 1NY, United Kingdom
    Endocr Rev 26:171-202. 2005

Collaborators

Detail Information

Publications38

  1. ncbi request reprint The role of 17beta-hydroxysteroid dehydrogenases in modulating the activity of 2-methoxyestradiol in breast cancer cells
    Simon P Newman
    Endocrinology and Metabolic Medicine, Faculty of Medicine, Imperial College, St Mary s Hospital, London, United Kingdom
    Cancer Res 66:324-30. 2006
    ..In addition, this study shows the value of synthesizing sulfamoylated derivatives of 2-MeOE2 with C17-position modifications as these compounds have improved bioavailability and potency both in vitro and in vivo...
  2. pmc Class III beta-tubulin expression and in vitro resistance to microtubule targeting agents
    C Stengel
    Oncology Drug Discovery and Women s Health Group, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 102:316-24. 2010
    ....
  3. pmc 2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer
    S L C Tagg
    Oncology Drug Discovery and Women s Health Group, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 99:1842-8. 2008
    ..This is the first study to show the benefit of combining a microtubule disruptor with 2DG in the two most common solid tumours...
  4. ncbi request reprint Eribulin, a simplified ketone analog of the tubulin inhibitor halichondrin B, for the potential treatment of cancer
    Simon Newman
    Endocrinology and Metabolic Medicine, and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, Norfolk Place, London W2 1NY, UK
    Curr Opin Investig Drugs 8:1057-66. 2007
    ..Eribulin is currently in phase II trials for NSCLC and soft tissue sarcoma, and pancreatic, prostate, ovarian, fallopian tube, peritoneal and head and neck cancer, and phase I/II trials for urothelial cancers...
  5. pmc The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers
    S P Newman
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 97:1673-82. 2007
    ..In contrast to the taxanes, STX140 can be dosed orally, with no toxicity being observed even after prolonged daily dosing...
  6. doi request reprint STX140 is efficacious in vitro and in vivo in taxane-resistant breast carcinoma cells
    Simon P Newman
    Endocrinology and Metabolic Medicine, Faculty of Medicine, Imperial College London, St Mary s Hospital, London, UK
    Clin Cancer Res 14:597-606. 2008
    ..In addition, its efficacy was determined against xenografts derived from patients who failed docetaxel therapy...
  7. ncbi request reprint Growth inhibition of multi-drug-resistant breast cancer cells by 2-methoxyoestradiol-bis-sulphamate and 2-ethyloestradiol-bis-sulphamate
    R N Suzuki
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 84:269-78. 2003
    ....
  8. ncbi request reprint The effects of 2-methoxyoestrogen sulphamates on the in vitro and in vivo proliferation of breast cancer cells
    T Utsumi
    Endocrinology and Metabolic Medicine, Imperial College Faculty of Medicine, St Mary s Hospital and Sterix Ltd, London, W2 1NY, UK
    J Steroid Biochem Mol Biol 94:219-27. 2005
    ....
  9. pmc The in vivo properties of STX243: a potent angiogenesis inhibitor in breast cancer
    M F C Parsons
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 99:1433-41. 2008
    ..These results show that STX243 is a potent in vivo drug and could be clinically effective at treating a number of oncological conditions...
  10. ncbi request reprint Steroid sulfatase: molecular biology, regulation, and inhibition
    M J Reed
    Endocrinology and Metabolic Medicine, Imperial College, St Mary s Hospital, London W2 1NY, United Kingdom
    Endocr Rev 26:171-202. 2005
    ..The development of potent STS inhibitors will allow investigation of the role of this enzyme in physiological and pathological processes...
  11. ncbi request reprint Steroid sulphatase inhibitors for breast cancer therapy
    A Purohit
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 86:423-32. 2003
    ..Second generation inhibitors, such as 2-MeOE2bisMATE, which also inhibit the growth of ER- tumours should be active against a wide range of cancers...
  12. ncbi request reprint The effects of 2-methoxy oestrogens and their sulphamoylated derivatives in conjunction with TNF-alpha on endothelial and fibroblast cell growth, morphology and apoptosis
    Y T Ho
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 86:189-96. 2003
    ....
  13. ncbi request reprint Inhibition of oestrone sulphatase activity by tibolone and its metabolites
    A Purohit
    Dept of Endocrinology and Metabolic Medicine, Imperial College School of Medicine, St Mary s Hospital, London, W2 1NY, UK
    Horm Metab Res 34:1-6. 2002
    ..Results from this study have confirmed that tibolone and its metabolites can inhibit E1-STS activity. This may explain the absence of breast stimulation as observed in clinical studies...
  14. pmc 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
    J M Day
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 100:476-86. 2009
    ..This is despite an increase in BCRP expression in A2780 cells in vitro after chronic dosing with STX140...
  15. pmc In vivo inhibition of angiogenesis by sulphamoylated derivatives of 2-methoxyoestradiol
    S K Chander
    Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 96:1368-76. 2007
    ..This, together with their ability to inhibit tumour growth, indicates the potential of this new class of drugs for further development for cancer therapy...
  16. pmc Pharmacokinetics and efficacy of 2-methoxyoestradiol and 2-methoxyoestradiol-bis-sulphamate in vivo in rodents
    C R Ireson
    1Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Br J Cancer 90:932-7. 2004
    ..The resistance to metabolism shown by 2-MeOE2bisMATE and its ability to inhibit tumour growth in vivo suggest that this compound should have considerable potential for development as a novel anticancer drug...
  17. ncbi request reprint The regulation and inhibition of 17beta-hydroxysteroid dehydrogenase in breast cancer
    A Purohit
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Mol Cell Endocrinol 248:199-203. 2006
    ..The identification of potent, selective novel 17beta-HSD1 inhibitors will allow their efficacy to be tested in in vitro and in vivo studies...
  18. ncbi request reprint Cofactor competition between the ligand-bound oestrogen receptor and an intron 1 enhancer leads to oestrogen repression of ERBB2 expression in breast cancer
    S P Newman
    ICRF Molecular Oncology Unit, ICSM Hammersmith Hospital, London, UK
    Oncogene 19:490-7. 2000
    ....
  19. ncbi request reprint Regulation of steroid sulphatase expression and activity in breast cancer
    S P Newman
    Endocrinology and Metabolic Medicine, Imperial College School of Medicine, St Mary s Hospital, W2 1NY, London, UK
    J Steroid Biochem Mol Biol 75:259-64. 2000
    ..In conjunction with the lack of regulation of STS mRNA it suggest that TNFalpha and IL-6 may increase STS activity via a post-translational modification of the enzyme or by increasing substrate availability...
  20. ncbi request reprint Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates
    Y T Ho
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Biochem Biophys Res Commun 305:909-14. 2003
    ....
  21. ncbi request reprint 17Beta-hydroxysteroid dehydrogenase Type 1 and Type 2: association between mRNA expression and activity in cell lines
    Joanna M Day
    Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Mol Cell Endocrinol 248:246-9. 2006
    ..An understanding of their regulation in both healthy and malignant tissues may lead to future therapeutic intervention at the regulatory level...
  22. doi request reprint Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents
    Mathew P Leese
    Department of Pharmacy and Pharmacology, University of Bath, Bath, UK
    J Med Chem 51:1295-308. 2008
    ..The potential of these multimechanism anticancer agents was confirmed in vivo, with promising activity observed for both 14 and 15 in an athymic nude mouse MDA-MB-231 human breast cancer xenograft model...
  23. ncbi request reprint A new micronized formulation of 2-methoxyestradiol-bis-sulfamate (STX140) is therapeutically potent against breast cancer
    Paul A Foster
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Anticancer Res 28:577-81. 2008
    ..A new micronized formulation of STX140 has now been developed and its pharmacokinetics (PK) in rats and effect on MDA-MB-231 breast cancer growth in nude mice was investigated...
  24. ncbi request reprint A comparison of two orally bioavailable anti-cancer agents, IRC-110160 and STX140
    Paul A Foster
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, UK
    Anticancer Res 28:1483-91. 2008
    ..This study characterises two recently developed anticancer agents in vitro and in vivo, 2-methoxyoestra-1,3,5(10), 16-tetraene-3-carboxamide (IRC-110160) and STX140...
  25. doi request reprint IRC-083927 is a new tubulin binder that inhibits growth of human tumor cells resistant to standard tubulin-binding agents
    Anne Marie Liberatore
    Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, Les Ulis, France
    Mol Cancer Ther 7:2426-34. 2008
    ....
  26. ncbi request reprint The effects of 2-substituted oestrogen sulphamates on the growth of prostate and ovarian cancer cells
    Joanna M Day
    Endocrinology and Metabolic Medicine, Faculty of Medicine and Sterix Ltd, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 84:317-25. 2003
    ....
  27. pmc The role of cytokines in regulating estrogen synthesis: implications for the etiology of breast cancer
    Atul Purohit
    Faculty of Medicine, Imperial College, St Mary s Hospital, London, UK
    Breast Cancer Res 4:65-9. 2002
    ..The co-ordinated stimulation of the activities of the enzymes that are involved in estrogen synthesis offers an explanation for the high concentrations of estrogens that are present in breast tumors...
  28. doi request reprint 17beta-hydroxysteroid dehydrogenase Type 1, and not Type 12, is a target for endocrine therapy of hormone-dependent breast cancer
    Joanna M Day
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College London, St Mary s Hospital, London W2 1NY, United Kingdom
    Int J Cancer 122:1931-40. 2008
    ..Both E2 production and tumor growth were inhibited by STX1040, suggesting that 17beta-HSD1 inhibitors such as STX1040 may provide a novel treatment for hormone-dependent breast cancer...
  29. doi request reprint Effects of mutations and glycosylations on STS activity: a site-directed mutagenesis study
    Chloe Stengel
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College London, St Mary s Hospital, London, W2 1NY, UK
    Mol Cell Endocrinol 283:76-82. 2008
    ..In addition, a polyclonal antibody raised in rabbits against human STS was developed and characterised. These data increase our knowledge of the STS enzyme structure and may help design new STS inhibitors...
  30. ncbi request reprint A-ring-substituted estrogen-3-O-sulfamates: potent multitargeted anticancer agents
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, U K
    J Med Chem 48:5243-56. 2005
    ..The potential of this novel class of multimechanism anticancer agents was confirmed in vivo with good activity observed in the NCI hollow fiber assay and in a MDA-MB-435 xenograft mouse model...
  31. ncbi request reprint 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, United Kingdom
    J Med Chem 49:7683-96. 2006
    ..2-Substituted E2bisMATEs are attractive candidates for further development as multitargeted anticancer agents...
  32. ncbi request reprint Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, UK
    J Steroid Biochem Mol Biol 94:239-51. 2005
    ..The SAR parameters established herein will assist the future design of anti-proliferative and anti-endocrine agents as potential therapeutics for both hormone dependent and independent cancers...
  33. ncbi request reprint 3,17-disubstituted 2-alkylestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anticancer activity
    Christian Bubert
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    J Med Chem 50:4431-43. 2007
    ..3-O-Sulfamoylated 2-alkylestradiol-17-O-carbamates and sulfamates have considerable potential as anticancer agents...
  34. ncbi request reprint Efficacy of three potent steroid sulfatase inhibitors: pre-clinical investigations for their use in the treatment of hormone-dependent breast cancer
    Paul A Foster
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College Faculty of Medicine, St Mary s Hospital, London, W2 1NY, UK
    Breast Cancer Res Treat 111:129-38. 2008
    ..This study indicates that the STS inhibitor, STX213, exhibits excellent efficacy and pharmacokinetics and therefore offers a potentially novel treatment for hormone-dependent breast cancer...
  35. ncbi request reprint 2-MeOE2bisMATE and 2-EtE2bisMATE induce cell cycle arrest and apoptosis in breast cancer xenografts as shown by a novel ex vivo technique
    Paul A Foster
    Faculty of Medicine, Imperial College London, St Mary s Hospital, London, W2 1NY, UK
    Breast Cancer Res Treat 111:251-60. 2008
    ..As these compounds are anti-proliferative against breast cancer and endothelial cells they have the potential to be potent, dual acting clinical drugs of the future...
  36. ncbi request reprint 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem Lett 14:3135-8. 2004
    ....
  37. ncbi request reprint Inhibition of in vitro angiogenesis by 2-methoxy- and 2-ethyl-estrogen sulfamates
    Simon P Newman
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London, United Kingdom
    Int J Cancer 109:533-40. 2004
    ..The sulfamoylated derivatives of 2-MeOE2 and 2-EtE2 are potent inhibitors of in vitro angiogenesis and both compounds should have therapeutic potential...
  38. ncbi request reprint In vivo efficacy of STX213, a second-generation steroid sulfatase inhibitor, for hormone-dependent breast cancer therapy
    Paul A Foster
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College Faculty of Medicine, St Mary s Hospital, London, United Kingdom
    Clin Cancer Res 12:5543-9. 2006
    ..We compare the in vivo efficacy of two potent STS inhibitors, STX64 and STX213, in a xenograft breast cancer model...