- Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy
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Triple negative breast cancer (TNBC) is an aggressive disease with high relapse rates and few treatment options. Outlined in previous publications, we identified a series of potent, dual TTK/CLK2 inhibitors with strong efficacy in TNBC xenograft models. P
- Riggs, Jennifer R.,Elsner, Jan,Cashion, Dan,Robinson, Dale,Tehrani, Lida,Nagy, Mark,Fultz, Kimberly E.,Krishna Narla, Rama,Peng, Xiaohui,Tran, Tam,Kulkarni, Ashutosh,Bahmanyar, Sogole,Condroski, Kevin,Pagarigan, Barbra,Fenalti, Gustavo,Lebrun, Laurie,Leftheris, Katerina,Zhu, Dan,Boylan, John F.
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supporting information
p. 4401 - 4410
(2019/05/17)
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- Highly efficient conversion of alcohols to isocyanides
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Treatment of tertiary alcohols with silver salts (AgClO4, AgBF4, or AgOTf) and trimethylsilyl cyanide (TMSCN), followed by hydrolysis, directly affords excellent yields of corresponding isocyanides. This reaction proceeds selectively
- Kitano,Chiba,Tada
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p. 437 - 443
(2007/10/03)
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- SULFUR YLIDES IN REACTIONS WITH 4-SUBSTITUTED CYCLOHEXANONES: STEREOCHEMISTRY AND REACTIVITY
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The stereochemistry of the epoxidation reactions of the title compounds (R= Me, Et, t-Bu, Ph, p-F-Ph, OMe, OH, CF3, OCOPh) with sulfur ylides (dimethylsulfonium methylide and dimethyloxosulfonium methylide) has been determined in three different solvents (DMSO, C6H6 and THF).Relative rates have been measured and the kinetic constants kcis and ktrans determined.
- Migneco, Luisa M.,Vecchi, Elisabetta
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- SYNTHESIS OF CIS- AND TRANS-1-METHYLCYCLOHEXANE-1,4-DIOLS AND THEIR 4-HEMISUCCINATE ESTERS
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Stereoselective syntheses of the previously uncharacterized cis- and trans-1-methylcyclohexane-1,4-diols and their conversion to 4-hemisuccinate esters are described.
- Bushweller, John H.,Anzalone, Luigi,Spencer, Thomas A.
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p. 745 - 754
(2007/10/02)
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