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• W2097472327 endingPage "12267" @default.
• W2097472327 startingPage "12256" @default.
• W2097472327 abstract "Abstract The methyl group is one of the most commonly occurring carbon fragments in small‐molecule drugs. This simplest alkyl fragment appears in more than 67 % of the top‐selling drugs of 2011 and can modulate both the biological and physical properties of a molecule. This Review focuses on so‐called magic methyl effects on binding potency, where the seemingly mundane change of CH to CMe improves the IC 50 value of a drug candidate more than 100‐fold. This discussion is followed by a survey of recent advances in synthetic chemistry that allow the direct methylation of C(sp 2 )H and C(sp 3 )H bonds. It is our hope that the relevance of the meager methyl group to drug discovery as presented herein will inspire reports on new CH methylation reactions." @default.
• W2097472327 created "2016-06-24" @default.
• W2097472327 creator A5056853464 @default.
• W2097472327 creator A5081078298 @default.
• W2097472327 date "2013-10-22" @default.
• W2097472327 modified "2023-10-18" @default.
• W2097472327 title "Profound Methyl Effects in Drug Discovery and a Call for New CH Methylation Reactions" @default.
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