Triazole-based inhibitors of geranylgeranyltransferase II

…, SV Hartman, EJ Born, JP Smits, SA Holstein…

Index: Zhou, Xiang; Hartman, Sara V.; Born, Ella J.; Smits, Jacqueline P.; Holstein, Sarah A.; Wiemer, David F. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 3 p. 764 - 766

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Citation Number: 14

Abstract

A small set of triazole bisphosphonates has been prepared and tested for the ability to inhibit geranylgeranyltransferase II (GGTase II). The compounds were prepared through use of click chemistry to assemble a central triazole that links a polar head group to a hydrophobic tail. The resulting compounds were tested for their ability to inhibit GGTase II in an in vitro enzyme assay and also were tested for cytotoxic activity in an MTT assay with the human ...