Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

Sabbir Ahmed, Chirag K. Patel

Research output: Contribution to journalArticlepeer-review

Abstract

We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.
Original languageEnglish
Pages (from-to)437-443
Number of pages7
JournalLetters in Drug Design & Discovery
Volume11
Issue number4
Publication statusPublished - 1 May 2014
Externally publishedYes

Keywords

  • estrone sulfatase
  • irreversible
  • inhibition
  • breast cancer
  • isophthanoic acid esters
  • electron density
  • ES inhibitor

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