64605-33-0Relevant academic research and scientific papers
Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor
Tjin, Caroline Chandra,Wissner, Rebecca F.,Jamali, Haya,Schepartz, Alanna,Ellman, Jonathan A.
, p. 1013 - 1018 (2018)
Protein arginine deiminase 4 (PAD4) is a calcium-dependent enzyme that catalyzes the conversion of arginine to citrulline within target proteins. Dysregulation of PAD4 has been implicated in a number of human diseases, including rheumatoid arthritis and other inflammatory diseases as well as cancer. In this study, we report on the design, synthesis, and evaluation of a new class of haloacetamidine-based compounds as potential PAD4 inhibitors. Specifically, we describe the identification of 4,5,6-trichloroindazole 24 as a highly potent PAD4 inhibitor that displays >10-fold selectivity for PAD4 over PAD3 and >50-fold over PAD1 and PAD2. The efficacy of this compound in cells was determined by measuring the inhibition of PAD4-mediated H4 citrullination in HL-60 granulocytes.
SIMPLE SYNTHESIS OF 3-ALKYL-1H-INDAZOLES HAVING FUNCTIONAL GROUPS AT THE ω-POSITION
Sasakura, Kazuyuki,Kawasaki, Akiko,Sugasawa, Tsutomu
, p. 259 - 264 (2007/10/02)
3-Alkyl-1H-indazoles (1) having a functional group at the ω-position can be simply synthesized by using 2-(ω-chloroalkanoyl)anilines (3) as starting material.
