Krüppel-like Factor 5 (KLF5), a Zn finger-containing transcription factor implicated in colorectal cancer (CRC), is a strong promoter of cell growth and angiogenesis. KLF5 is not only abundant in many types of CRCs, it also promotes growth when added to tumor cell cultures. This report shows an HTS-based effort to find small molecules that suppress KLF5 expression, optimization of one series for <i>in vivo</i> use, and the finding that an optimized analog, ML264, promotes CRC cell death. This activity is seen both in cell culture and in tumor xenograft studies in mice. SAR and further structural changes in the series are also discussed.

Small molecule KLF5 inhibitors: New agents for treating colorectal cancers

251st National Meeting (2016)

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