Letters in Drug Design & Discovery

Author(s): Chirag K. Patel and Sabbir Ahmed

DOI: 10.2174/157018011793663967

Synthesis and In Vitro Biochemical Evaluation of a Series of Alkyl 6- Aminosulfonyl Naphthanoates as Potential Inhibitors of Human Placental Estrone Sulfatase (ES)

Page: [26 - 31] Pages: 6

  • * (Excluding Mailing and Handling)

Abstract

We report the tentative initial results of our on-going search for potent inhibitors of estrone sulfatase (ES), here we report a series of alkyl 6-aminosulfonyl naphthanoate-based compounds as potential inhibitors. The results suggest that the compounds are weak inhibitors in comparison to the standard compound used within the current study.

Keywords: Estrone sulfatase, Inhibition, Irreversible, Breast cancer, Naphthanoic acid esters, aromatase, AR, estrone, estradiol, EMATE, EPSRC Mass Spectrometry, temperature, Melting points, DMA, TRITONX, TLC, 1HNMR, clogP, Benzoates, Non-Sulfamoylated Derivative, COUMATE, inhibitors, alkyl chain, substrate, transition-state, hydrophobicity, IC50