Literature DB >> 20386818

Chimeric microtubule disruptors.

Mathew P Leese1, Fabrice Jourdan, Meriel R Kimberley, Gyles E Cozier, Nethaji Thiyagarajan, Chloe Stengel, Sandra Regis-Lydi, Paul A Foster, Simon P Newman, K Ravi Acharya, Eric Ferrandis, Atul Purohit, Michael J Reed, Barry V L Potter.   

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.

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Year:  2010        PMID： 20386818     DOI： 10.1039/c002558e

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  10 in total

1.  Tetrahydroisoquinolinone-based steroidomimetic and chimeric microtubule disruptors.

Authors:  Mathew P Leese; Fabrice L Jourdan; Meriel R Major; Wolfgang Dohle; Ernest Hamel; Eric Ferrandis; Ann Fiore; Philip G Kasprzyk; Barry V L Potter
Journal:  ChemMedChem       Date:  2013-10-09       Impact factor: 3.466

2.  Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.

Authors:  Mark P Thomas; Barry V L Potter
Journal:  J Med Chem       Date:  2015-06-12       Impact factor: 7.446

3.  Optimisation of tetrahydroisoquinoline-based chimeric microtubule disruptors.

Authors:  Wolfgang Dohle; Mathew P Leese; Fabrice L Jourdan; Christopher J Chapman; Ernest Hamel; Eric Ferrandis; Barry V L Potter
Journal:  ChemMedChem       Date:  2014-05-12       Impact factor: 3.466

4.  Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.

Authors:  Mathew P Leese; Fabrice Jourdan; Wolfgang Dohle; Meriel R Kimberley; Mark P Thomas; Ruoli Bai; Ernest Hamel; Eric Ferrandis; Barry V L Potter
Journal:  ACS Med Chem Lett       Date:  2011-10-31       Impact factor: 4.345

5.  Targeted NF1 cancer therapeutics with multiple modes of action: small molecule hormone-like agents resembling the natural anticancer metabolite, 2-methoxyoestradiol.

Authors:  Yu-chi Shen; Ravi Upadhyayula; Stephanie Cevallos; Ryan J Messick; Tammy Hsia; Mathew P Leese; Douglas M Jewett; Daysha Ferrer-Torres; Therese M Roth; Wolfgang Dohle; Barry V L Potter; Kate F Barald
Journal:  Br J Cancer       Date:  2015-10-13       Impact factor: 7.640

6.  Accessing simply-substituted 4-hydroxytetrahydroisoquinolines via Pomeranz-Fritsch-Bobbitt reaction with non-activated and moderately-activated systems.

Authors:  Marco Mottinelli; Mathew P Leese; Barry V L Potter
Journal:  Beilstein J Org Chem       Date:  2017-09-06       Impact factor: 2.883

7.  Modes of cell death induced by tetrahydroisoquinoline-based analogs in MDA-MB-231 breast and A549 lung cancer cell lines.

Authors:  Marcel Nel; Anna M Joubert; Wolfgang Dohle; Barry Vl Potter; Anne E Theron
Journal:  Drug Des Devel Ther       Date:  2018-06-25       Impact factor: 4.162

8.  Nonsteroidal sulfamate derivatives as new therapeutic approaches for Neurofibromatosis 2 (NF2).

Authors:  Yu-Chi Shen; Caroline Arellano-Garcia; Rosa E Menjivar; Ethan M Jewett; Wolfgang Dohle; Sofiia Karchugina; Jonathan Chernoff; Barry V L Potter; Kate F Barald
Journal:  BMC Pharmacol Toxicol       Date:  2019-11-15       Impact factor: 2.483

9.  Synthesis, anti-tubulin and antiproliferative SAR of steroidomimetic dihydroisoquinolinones.

Authors:  Mathew P Leese; Fabrice L Jourdan; Meriel R Major; Wolfgang Dohle; Mark P Thomas; Ernest Hamel; Eric Ferrandis; Mary F Mahon; Simon P Newman; Atul Purohit; Barry V L Potter
Journal:  ChemMedChem       Date:  2014-03-05       Impact factor: 3.466

10.  In vivo and in vitro properties of STX2484: a novel non-steroidal anti-cancer compound active in taxane-resistant breast cancer.

Authors:  C Stengel; S P Newman; J M Day; S K Chander; F L Jourdan; M P Leese; E Ferrandis; S Regis-Lydi; B V L Potter; M J Reed; A Purohit; P A Foster
Journal:  Br J Cancer       Date:  2014-06-24       Impact factor: 7.640
  10 in total

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