Showing papers by "Sukwon Hong published in 2010"
TL;DR: C(1)-symmetric isoquinoline-based chiral diaminocarbene ligands (MIQ) have been developed to block three quadrants of the metal coordination sphere, complementing C(2)-Symmetric biisoquinoline (BIQ) ligands.
79 citations
TL;DR: Base-functionalized aza-bis(oxazoline) ligands were prepared to explore the concept of dual activation through the Lewis acid and a tethered tertiary amine base to improve enantioselectivity and rate acceleration.
Abstract: Base-functionalized aza-bis(oxazoline) ligands were prepared to explore the concept of dual activation through the Lewis acid and a tethered tertiary amine base. The catalytic activity of the Cu complex was evaluated for the asymmetric Henry reaction. Compared with a corresponding unfunctionalized copper complex with external 1-benzyl-4-ethylpiperazine base, the ethylpiperazine-functionalized aza-bis(oxazoline) copper catalyst resulted in rate acceleration (2.5 times) as well as improved enantioselectivity (72% ee vs 92% ee).
69 citations
TL;DR: Sterically demanding and conformationally stable N,N'-ditertiaryalkyl-N,N,'diphenyl acyclic diaminocarbenes (ADCs) were developed and demonstrated unique ligand properties different from bulky N-heterocyclic carbene (NHC) counterparts.
63 citations
TL;DR: In this paper, 2-Alkylpyrrolidines were used as building blocks for acyclic diaminocarbenes (ADCs), and the ability of these ligands to direct stereochemistry and enhance activity was explored in the Suzuki cross-coupling reaction and the 1,2 addition of arylboronic acids to aldehydes.
44 citations
TL;DR: One compound was identified that inhibits wild-type protease, as well as a drug-resistant protease with six mutations that suggests an allosteric non-competitive mechanism of inhibition and may represent a starting point for an additional strategy for anti-retroviral therapy.
Abstract: Clinically approved inhibitors of the HIV-1 protease function via a competitive mechanism. A particular vulnerability of competitive inhibitors is their sensitivity to increases in substrate concentration, as may occur during virion assembly, budding and processing into a mature infectious viral particle. Advances in chemical synthesis have led to the development of new high-diversity chemical libraries using rapid in-solution syntheses. These libraries have been shown previously to be effective at disrupting protein-protein and protein-nucleic acid interfaces. We have screened 44000 compounds from such a library to identify inhibitors of the HIV-1 protease. One compound was identified that inhibits wild-type protease, as well as a drug-resistant protease with six mutations. Moreover, analysis of this compound suggests an allosteric non-competitive mechanism of inhibition and may represent a starting point for an additional strategy for anti-retroviral therapy.
19 citations