Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

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


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.

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

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Article Details

Year: 2006
Page: [44 - 48]
Pages: 5
DOI: 10.2174/157018006775240890