We are excited to share a groundbreaking development in cancer research through our enduring collaboration with Professors Kevin Pinney and Mary Lynn Trawick at Baylor University. The recently published study, led by Wen Ren, explores the Synthesis and biological evaluation of structurally diverse 6-aryl-3-aroyl-indole analogues as inhibitors of tubulin polymerization.
In our latest collaborative effort, Wen Ren, in partnership with Mason Lab and Baylor University, delves into the synthesis and evaluation of small-molecule inhibitors of tubulin polymerization. Focused on the colchicine site of the tubulin heterodimer, the study builds upon previous discoveries, particularly the potent 2-aryl-3-aroyl-indole analogue (OXi8006).
The research led to the development of several structurally diverse 6-aryl-3-aroyl-indole analogues. Among them, KGP591 demonstrated significant promise, inducing G2/M arrest in MDA-MB-231 cells, disrupting microtubule structure, and exhibiting notable inhibition of cell migration.
The phosphate prodrug salt of KGP591, KGP618, displayed substantial reduction in bioluminescence signal in vivo, indicating vascular disrupting agent (VDA) efficacy in an orthotopic model of kidney cancer (RENCA-luc) in BALB/c mice.
While Wen Ren spearheaded this study, our collaborative efforts between Mason Lab and Baylor University underscore the potential of these tubulin polymerization inhibitors as innovative anticancer therapeutic agents.
This breakthrough not only contributes valuable insights to the field but also reflects our commitment to advancing cancer therapeutics through collaborative and interdisciplinary research. Mason Lab is proud to be at the forefront of pioneering cancer research in partnership with Baylor University, and we look forward to future strides in transformative discoveries.
Collaboration breeds innovation; together, Mason Lab and Baylor University advance the frontiers of cancer research.