Synthesis and phosphatase inhibitory activity of 3-alkynylestrones and their derivatives

Anton Ivanov; Sebastian Boldt; Zaib un Nisa; Syed Jawad Ali Shah; Peter Ehlers; Alexander Villinger; Gyula Schneider; János Wölfling; Qamar Rahman; Jamshed Iqbal; Peter Langer

doi:10.1039/C5RA25558A

Synthesis and phosphatase inhibitory activity of 3-alkynylestrones and their derivatives†

Anton Ivanov,^a Sebastian Boldt,^a Zaib un Nisa,^b Syed Jawad Ali Shah,^b Peter Ehlers,^ac Alexander Villinger,^a Gyula Schneider,^d János Wölfling,^d Qamar Rahman,^ae Jamshed Iqbal^b and Peter Langer*^ac

Author affiliations

* Corresponding authors

^a Institut für Chemie, Universität Rostock, Albert Einstein Str. 3a, 18059 Rostock, Germany
E-mail: peter.langer@uni-rostock.de

^b Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad, Pakistan

^c Leibniz-Institut für Katalyse an der Universität Rostock e.V., Albert Einstein Str. 29a, 18059 Rostock, Germany

^d Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary

^e Amity University, Lucknow Campus, Viraj Khand-5, Gomti Nagar, Lucknow-226010, India

Abstract

A range of 3-alkynylated 3-deoxy-estrones were prepared by Sonogashira reactions and transformed into estrone derived diones and quinoxalines. The alkynylated estrones and their derivatives exhibit significant biological activity as alkaline phosphatase inhibitors. The mode of action was illustrated based on docking studies.

RSC Advances

Synthesis and phosphatase inhibitory activity of 3-alkynylestrones and their derivatives†

Abstract

Supplementary files

Article information

Download Citation

Author version available

Permissions

Synthesis and phosphatase inhibitory activity of 3-alkynylestrones and their derivatives

Social activity

Search articles by author

Spotlight

Advertisements