Initial Design and Synthesis of Conformationally Restricted and Pharmacophore-Based Scaffold Hopping Analogs of a Ras Pathway Modulator and Evaluation of Their MAPK Inhibitory Activities

The initial design and synthesis of conformationally restricted and pharmacophore-based scaffold hopping analogs of a Ras/Raf protein interaction inhibitor were undertaken with the objective of identifying alternate chemical scaffolds exhibiting similar biological activities. Evaluation of the MAPK pathway signaling inhibitory activity and antiproliferative activity of the synthesized derivatives were performed.