A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness.

@article{Barcelos2014ANG,
  title={A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness.},
  author={Rosimeire Coura Barcelos and Karin Juliane Pelizzaro-Rocha and Julio C Pastre and Marina Pereira Dias and Carmen Ver{\'i}ssima Ferreira-Halder and Ronaldo A Pilli},
  journal={European journal of medicinal chemistry},
  year={2014},
  volume={87},
  pages={745-58}
}
In this study, a novel concise series of molecules based on the structure of goniothalamin (1) was synthesized and evaluated against a highly metastatic human pancreatic cancer cell line (Panc-1). Among them, derivative 8 displayed a low IC50 value (2.7 μM) and its concentration for decreasing colony formation was 20-fold lower than goniothalamin (1). Both compounds reduced the levels of the receptor tyrosine kinase (AXL) and cyclin D1 which are known to be overexpressed in pancreatic cancer… CONTINUE READING
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