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Chimeric microtubule disruptors.

Leese MP, Jourdan F, Kimberley MR, Cozier GE, Thiyagarajan N, Stengel C, Regis-Lydi S, Foster PA, Newman SP, Acharya KR, Ferrandis E, Purohit A, Reed MJ, Potter BV
Chem Commun (Camb) 46 2907-9 (2010)
Cited: 13 times
EuropePMC logo PMID: 20386818

Abstract

A chimeric approach is used to discover microtubule disruptors with excellent in vitro activity and oral bioavailability; a ligand-protein interaction with carbonic anhydrase that enhances bioavailability is characterised by protein X-ray crystallography. Dosing of a representative chimera in a tumour xenograft model confirms the excellent therapeutic potential of the class.

Articles - 2wd2 mentioned but not cited (1)

  1. Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations. De Simone G, Langella E, Esposito D, Supuran CT, Monti SM, Winum JY, Alterio V. J Enzyme Inhib Med Chem 32 1002-1011 (2017)


Reviews citing this publication (3)

  1. Recent Advances in chemistry and pharmacology of 2-methoxyestradiol: An anticancer investigational drug. Kumar BS, Raghuvanshi DS, Hasanain M, Alam S, Sarkar J, Mitra K, Khan F, Negi AS. Steroids 110 9-34 (2016)
  2. Sulfatase inhibitors: a patent review. Williams SJ. Expert Opin Ther Pat 23 79-98 (2013)
  3. Thermodynamic, kinetic, and structural parameterization of human carbonic anhydrase interactions toward enhanced inhibitor design. Linkuvienė V, Zubrienė A, Manakova E, Petrauskas V, Baranauskienė L, Zakšauskas A, Smirnov A, Gražulis S, Ladbury JE, Matulis D. Q Rev Biophys 51 e10 (2018)

Articles citing this publication (9)

  1. Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors. Leese MP, Jourdan F, Dohle W, Kimberley MR, Thomas MP, Bai R, Hamel E, Ferrandis E, Potter BV. ACS Med Chem Lett 3 5-9 (2012)
  2. Tetrahydroisoquinolinone-based steroidomimetic and chimeric microtubule disruptors. Leese MP, Jourdan FL, Major MR, Dohle W, Hamel E, Ferrandis E, Fiore A, Kasprzyk PG, Potter BV. ChemMedChem 9 85-108, 1 (2014)
  3. Synthesis, antitubulin, and antiproliferative SAR of C3/C1-substituted tetrahydroisoquinolines. Dohle W, Leese MP, Jourdan FL, Major MR, Bai R, Hamel E, Ferrandis E, Kasprzyk PG, Fiore A, Newman SP, Purohit A, Potter BV. ChemMedChem 9 350-370 (2014)
  4. Tetrahydroisoquinoline Sulfamates as Potent Microtubule Disruptors: Synthesis, Antiproliferative and Antitubulin Activity of Dichlorobenzyl-Based Derivatives, and a Tubulin Cocrystal Structure. Dohle W, Prota AE, Menchon G, Hamel E, Steinmetz MO, Potter BVL. ACS Omega 4 755-764 (2019)
  5. Targeted NF1 cancer therapeutics with multiple modes of action: small molecule hormone-like agents resembling the natural anticancer metabolite, 2-methoxyoestradiol. Shen YC, Upadhyayula R, Cevallos S, Messick RJ, Hsia T, Leese MP, Jewett DM, Ferrer-Torres D, Roth TM, Dohle W, Potter BV, Barald KF. Br J Cancer 113 1158-1167 (2015)
  6. In vivo and in vitro properties of STX2484: a novel non-steroidal anti-cancer compound active in taxane-resistant breast cancer. Stengel C, Newman SP, Day JM, Chander SK, Jourdan FL, Leese MP, Ferrandis E, Regis-Lydi S, Potter BV, Reed MJ, Purohit A, Foster PA. Br J Cancer 111 300-308 (2014)
  7. Nonsteroidal sulfamate derivatives as new therapeutic approaches for Neurofibromatosis 2 (NF2). Shen YC, Arellano-Garcia C, Menjivar RE, Jewett EM, Dohle W, Karchugina S, Chernoff J, Potter BVL, Barald KF. BMC Pharmacol Toxicol 20 67 (2019)
  8. Accessing simply-substituted 4-hydroxytetrahydroisoquinolines via Pomeranz-Fritsch-Bobbitt reaction with non-activated and moderately-activated systems. Mottinelli M, Leese MP, Potter BVL. Beilstein J Org Chem 13 1871-1878 (2017)
  9. Quantitative Analysis of the Potency of Equimolar Two-Drug Combinations and Combi-Molecules Involving Kinase Inhibitors In Vitro: The Concept of Balanced Targeting. Rao S, Thibault B, Peyrard L, Larroque-Lombard AL, Rupp M, Thauvin C, Jean-Claude BJ. Int J Mol Sci 22 9569 (2021)


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