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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Sanjay R. Menon

Volume 3 , Issue 1 , 2006

Page: [44 - 48] Pages: 5

DOI: 10.2174/157018006775240890

Price: $65


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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