Subject Area

Chemistry

Description

The primary objective of this research is synthesizing derivatives of known Arp2/3 inhibitor CK-666 and to determine their potency of inhibition of the Actin Related Protein (Arp 2/3) complex. A potent Arp2/3 inhibitor may be of interest in clinical anti-cancer and anti-tumor applications. Additionally, an Arp2/3 inhibitor with nanomolar potency could be used to advance basic actin dynamics research. Herein the organic synthetic efforts towards the 2-methyl-7-azaindole derivative of the known Arp2/3 inhibitor CK-666 are described. Polymerization assays providing preliminary in vitro IC50 data are also discussed.

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May 17th, 12:00 AM

Synthesis and Preliminary Bioactivity of Potential Inhibitors of Arp 2/3 Complex

The primary objective of this research is synthesizing derivatives of known Arp2/3 inhibitor CK-666 and to determine their potency of inhibition of the Actin Related Protein (Arp 2/3) complex. A potent Arp2/3 inhibitor may be of interest in clinical anti-cancer and anti-tumor applications. Additionally, an Arp2/3 inhibitor with nanomolar potency could be used to advance basic actin dynamics research. Herein the organic synthetic efforts towards the 2-methyl-7-azaindole derivative of the known Arp2/3 inhibitor CK-666 are described. Polymerization assays providing preliminary in vitro IC50 data are also discussed.