2. Academic Validation
  3. 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents

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

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3135-8. doi: 10.1016/j.bmcl.2004.04.027.
Mathew P Leese 1,  Simon P Newman,  Atul Purohit,  Michael J Reed,  Barry V L Potter
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK.
PMID: 15149660 DOI: 10.1016/j.bmcl.2004.04.027
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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