Polymerization of actin filaments is necessary for cellular structure, shape, division, and motility. The actin related protein 2/3 complex (Arp 2/3) consists of seven protein subunits that allow for the polymerization of actin within a cell by providing a nucleation site. Inhibition of Arp 2/3 can lead to a slower rate of polymerization of branching actin filaments within a cell which leads to slower motility rates. Overexpression of the Arp 2/3 complex has been linked with metastatic cancerous cells. Based on these discoveries, the inhibition of Arp 2/3 is a potential anticancer treatment. The overall goal of this research is to synthesize small molecule inhibitors of Arp 2/3 that have IC50 values in the nanomolar range. The research described herein is to synthesize 7-azaindole derivatives of CK-666—a commercially-available Arp2/3 inhibitor—and determine the effect of the additional nitrogen atom on the molecule’s potency. The work on this compound thus far is focused on synthesizing the 2-methyl substituted azaindole starting material that is not commercially available.

Synthesis of small molecule 7-azaindole derivatives of CK-666 as potential inhibitors of Arp 2/3 protein complex

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.