Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety

Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to address severa...

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Veröffentlicht in:	ACS medicinal chemistry letters 2015-10, Vol.6 (12), p.1241-1246
Hauptverfasser:	Ndubaku, Chudi O., Crawford, James J., Drobnick, Joy, Aliagas, Ignacio, Campbell, David, Dong, Ping, Dornan, Laura M., Duron, Sergio, Epler, Jennifer, Gazzard, Lewis, Heise, Christopher E., Hoeflich, Klaus P., Jakubiak, Diana, La, Hank, Lee, Wendy, Lin, Baiwei, Lyssikatos, Joseph P., Maksimoska, Jasna, Marmorstein, Ronen, Murray, Lesley J., O’Brien, Thomas, Oh, Angela, Ramaswamy, Sreemathy, Wang, Weiru, Zhao, Xianrui, Zhong, Yu, Blackwood, Elizabeth, Rudolph, Joachim
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES hERG kinase inhibitor Letter oncology pKa
Online-Zugang:	Volltext
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