The Experts below are selected from a list of 312 Experts worldwide ranked by ideXlab platform
Dongsheng Zhu - One of the best experts on this subject based on the ideXlab platform.
-
2 amino 2 3 dihydro 1h indene 5 carboxamide based discoidin domain receptor 1 ddr1 inhibitors design synthesis and in vivo antipancreatic cancer efficacy
Journal of Medicinal Chemistry, 2019Co-Authors: Dongsheng Zhu, Huocong Huang, Daniel M Pinkas, Jinfeng Luo, Debolina Ganguly, Alice E Fox, Emily N Arner, Qiuping Xiang, Alex N BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.
Alex N Bullock - One of the best experts on this subject based on the ideXlab platform.
-
2 amino 2 3 dihydro 1h indene 5 carboxamide based discoidin domain receptor 1 ddr1 inhibitors design synthesis and in vivo antipancreatic cancer efficacy
Journal of Medicinal Chemistry, 2019Co-Authors: Dongsheng Zhu, Huocong Huang, Daniel M Pinkas, Jinfeng Luo, Debolina Ganguly, Alice E Fox, Emily N Arner, Qiuping Xiang, Alex N BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.
Daniel M Pinkas - One of the best experts on this subject based on the ideXlab platform.
-
2 amino 2 3 dihydro 1h indene 5 carboxamide based discoidin domain receptor 1 ddr1 inhibitors design synthesis and in vivo antipancreatic cancer efficacy
Journal of Medicinal Chemistry, 2019Co-Authors: Dongsheng Zhu, Huocong Huang, Daniel M Pinkas, Jinfeng Luo, Debolina Ganguly, Alice E Fox, Emily N Arner, Qiuping Xiang, Alex N BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.
-
2-amino-2, 3-dihydro-1H-indene-5-carboxamide-based discoidin domain receptors 1 (DDR1) inhibitors: design, synthesis, and in vivo anti-pancreatic cancer efficacy
'American Chemical Society (ACS)', 2019Co-Authors: Zhu D, Daniel M Pinkas, Huang H, Luo J, Ganguly D, Ae Fox, Arner E, Xiang Q, Tu Z-c, An BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial−mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer
Huocong Huang - One of the best experts on this subject based on the ideXlab platform.
-
2 amino 2 3 dihydro 1h indene 5 carboxamide based discoidin domain receptor 1 ddr1 inhibitors design synthesis and in vivo antipancreatic cancer efficacy
Journal of Medicinal Chemistry, 2019Co-Authors: Dongsheng Zhu, Huocong Huang, Daniel M Pinkas, Jinfeng Luo, Debolina Ganguly, Alice E Fox, Emily N Arner, Qiuping Xiang, Alex N BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.
Jinfeng Luo - One of the best experts on this subject based on the ideXlab platform.
-
2 amino 2 3 dihydro 1h indene 5 carboxamide based discoidin domain receptor 1 ddr1 inhibitors design synthesis and in vivo antipancreatic cancer efficacy
Journal of Medicinal Chemistry, 2019Co-Authors: Dongsheng Zhu, Huocong Huang, Daniel M Pinkas, Jinfeng Luo, Debolina Ganguly, Alice E Fox, Emily N Arner, Qiuping Xiang, Alex N BullockAbstract:A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd Value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory Concentration Value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.