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

Title: 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

Volume: 3 Issue: 1

Author(s): Sukumar Sakamuri, Quin-Zene Chen, Yingchun Lu, Yen-Fang Keng, Vladimir Khazak, Katrin Illgen, Silke Schabbert, Lutz Weber and Sanjay R. Menon

Affiliation:

Keywords: Ras/Raf protein interaction inhibitor, conformational restriction, pharmacophore-based scaffold hopping, MAPK signaling pathway

Abstract: 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.

Cite this article as:

Sakamuri Sukumar, Chen Quin-Zene, Lu Yingchun, Keng Yen-Fang, Khazak Vladimir, Illgen Katrin, Schabbert Silke, Weber Lutz and Menon R. Sanjay, 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, Letters in Drug Design & Discovery 2006; 3 (1) . https://dx.doi.org/10.2174/157018006775240890