Synthesis and Pharmacological Evaluation of N-(3-(1 H-Indol-4-yl)-5-(2-methoxyisonicotinoyl) phenyl) methanesulfonamide (LP-261), a Potent Antimitotic Agent

…, A Stojanovic, M Bukhtiyarova, K Williams…

Index: Shetty, Rupa S.; Lee, Younghee; Liu, Bin; Husain, Arifa; Joseph, Rhoda W.; Lu, Yixin; Nelson, David; Mihelcic, John; Chao, Wenchun; Moffett, Kristofer K.; Schumacher, Andreas; Flubacher, Dietmar; Stojanovic, Aleksandar; Bukhtiyarova, Marina; Williams, Ken; Lee, Kyoung-Jin; Ochman, Alexander R.; Saporito, Michael S.; Moore, William R.; Flynn, Gary A.; Dorsey, Bruce D.; Springman, Eric B.; Fujimoto, Ted; Kelly, Martha J. Journal of Medicinal Chemistry, 2011 , vol. 54, # 1 p. 179 - 200

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Citation Number: 16

Abstract

The synthesis and optimization of a series of orally bioavailable 1-(1 H-indol-4-yl)-3, 5- disubstituted benzene analogues as antimitotic agents are described. A functionalized dibromobenzene intermediate was used as a key scaffold, which when modified by sequential Suzuki coupling and Buchwald− Hartwig amination provided a flexible entry to 1, 3, 5-trisubstituted phenyl compounds. A 1 H-indol-4-yl moiety at the 1-position was ...