The Experts below are selected from a list of 9255 Experts worldwide ranked by ideXlab platform
Rui Wang - One of the best experts on this subject based on the ideXlab platform.
-
an asymmetric approach toward chiral multicyclic spirooxindoles from isothiocyanato oxindoles and unsaturated Pyrazolones by a chiral tertiary amine thiourea catalyst
Chemical Communications, 2013Co-Authors: Qiao Chen, Jinyan Liang, Shoulei Wang, Dong Wang, Rui WangAbstract:The first organocatalytic Michael-cyclization cascade reaction between isothiocyanato oxindoles and unsaturated Pyrazolones has been developed. The multicyclic spiro[oxindole/thiobutyrolactam/pyrazolone] core structures containing three contiguous stereogenic centers, including two spiro quaternary centers, were prepared with excellent diastereo- (up to >20 : 1) and enantioselectivities (up to 99% ee).
John P. Mallamo - One of the best experts on this subject based on the ideXlab platform.
-
1 2 3 thiadiazole substituted Pyrazolones as potent kdr vegfr 2 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
-
1,2,3-Thiadiazole substituted Pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
Rabindranath Tripathy - One of the best experts on this subject based on the ideXlab platform.
-
1 2 3 thiadiazole substituted Pyrazolones as potent kdr vegfr 2 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
-
1,2,3-Thiadiazole substituted Pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
Edward R. Bacon - One of the best experts on this subject based on the ideXlab platform.
-
1 2 3 thiadiazole substituted Pyrazolones as potent kdr vegfr 2 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
-
1,2,3-Thiadiazole substituted Pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
Thelma S. Angeles - One of the best experts on this subject based on the ideXlab platform.
-
1 2 3 thiadiazole substituted Pyrazolones as potent kdr vegfr 2 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
-
1,2,3-Thiadiazole substituted Pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2006Co-Authors: Rabindranath Tripathy, Arup K. Ghose, Jasbir Singh, Edward R. Bacon, Thelma S. Angeles, Shi X. Yang, Mark S. Albom, Lisa D. Aimone, Joseph L. Herman, John P. MallamoAbstract:KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted Pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new Pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of Pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the Pyrazolones with the hinge region of the KDR kinase.
