Optimization of non-ATP competitive CDK/cyclin groove inhibitors through REPLACE-mediated fragment assembly
A major challenge in drug discovery is to develop and improve methods for targeting protein-protein interactions. Further exemplification of the REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) strategy for generatin
Sodium borohydride-iodine mediated reduction of γ-lactam carboxylic acids followed by DDQ mediated oxidative aromatisation: a simple approach towards N-aryl-formylpyrroles and 1,3-diaryl-formylpyrroles
A simple methodology for the conversion of substituted N-aryl-γ-lactam 2/3-carboxylic acids to substituted N-aryl-2/3-formyl-pyrroles has been developed. Several N-aryl-γ-lactam 2/3-carboxylic acids were reduced to substituted (N-aryl-pyrroliden-2/3-yl)-m
Haldar, Pranab,Barman, Gopa,Ray, Jayanta K.
p. 3049 - 3056
(2007/10/03)
Sodium borohydride-iodine mediated reduction of γ-lactam carboxylic acids followed by DDQ mediated oxidative aromatisation: A facile entry to N-aryl-formylpyrroles
A simple methodology for the conversion of substituted N-aryl-γ- lactam 2/3-carboxylic acids to substituted N-aryl-2/3-formyl-pyrroles has been developed. Several N-aryl-γ-lactam 2/3-carboxylic acids were reduced to substituted (N-aryl-pyrrolidine-2/3-yl)
Haldar, Pranab,Guin, Joyram,Ray, Jayanta K.
p. 1071 - 1074
(2007/10/03)
Novel HIV-1 protease inhibitors active against multiple PI-Resistant viral strains: Coadministration with indinavir
HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P 3 position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment.
Kevin, Nancy J.,Duffy, Joseph L.,Kirk, Brian A.,Chapman, Kevin T.,Schleif, William A.,Olsen, David B.,Stahlhut, Mark,Rutkowski, Carrie A.,Kuo, Lawrence C.,Jin, Lixia,Lin, Jiunn H.,Emini, Emilio A.,Tata, James R.
p. 4027 - 4030
(2007/10/03)
SYNTHESIS OF 1-SUBSTITUTED PYRROLE-3-CARBOXALDEHYDES
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Hamdan, Ali,Wasley, Jan W. F.
p. 741 - 744
(2011/02/21)
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