Literature DB >> 15149660

2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.

Mathew P Leese1, Simon P Newman, Atul Purohit, Michael J Reed, Barry V L Potter.   

Abstract

A flexible, direct, high yielding synthesis of 2-alkylsulfanyl estrogens from estrone has been developed. 2-Methylsulfanyl estradiol (2-MeSE2) 7 displays a similar anti-proliferative activity to the established 2-methoxyestradiol (2-MeOE2) 1, whilst its 3-O-sulfamate derivative (2-MeSE2MATE) 9 exhibits greatly enhanced anti-proliferative activity, combined with significant inhibition of steroid sulfatase, an enzyme target for the treatment of hormone-dependent tumours.

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Year:  2004        PMID： 15149660     DOI： 10.1016/j.bmcl.2004.04.027

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 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.  A sequential, multiple-treatment, targeted approach to reduce wound healing and failure of glaucoma filtration surgery in a rabbit model (an American Ophthalmological Society thesis).

Authors:  Mark Brian Sherwood
Journal:  Trans Am Ophthalmol Soc       Date:  2006

4.  Neurosteroid Analogues. 13. Synthetic methods for the preparation of 2beta-hydroxygonane derivatives as structural mimics of ent-3alpha-hydroxysteroid modulators of GABA(A) receptors.

Authors:  Cunde Wang; Nigam P Rath; Douglas F Covey
Journal:  Tetrahedron       Date:  2007-08-13       Impact factor: 2.457

5.  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

6.  Molecular crosstalk between apoptosis and autophagy induced by a novel 2-methoxyestradiol analogue in cervical adenocarcinoma cells.

Authors:  Anne E Theron; Elsie M Nolte; Laurence Lafanechère; Annie M Joubert
Journal:  Cancer Cell Int       Date:  2013-08-27       Impact factor: 5.722
  6 in total

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