Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Julia, Cajica"'
Autor:
Allister Fraser, Kevin R. Shreder, Junichi Ishiyama, John W. Kozarich, Yi Hu, Yasushi Kohno, Heidi E. Brown, Lingling Du, Eric Okerberg, Christopher M. Amantea, Julia Cajica, Emme C.K. Lin, Lan M. Pham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1553-1556
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn2+-dependent, 27 nM inhibitor of human plasma Lp-PLA2. Structure–activity relationship studies focused on the AX10479 2-phenylamide gro
Autor:
Eric Okerberg, Julia Cajica, Kevin R. Shreder, Yasushi Kohno, Lan M. Pham, Heidi E. Brown, Junichi Ishiyama, Yi Hu, John W. Kozarich, Allister Fraser, Lingling Du, Emme C.K. Lin, Christopher M. Amantea
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:868-871
AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100 nM inhibitor of Lp-PLA2. However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA2 did not change. Subsequent
Autor:
Po-Shen Pan, Shelli R. McAlpine, Irene Medina, Ricardo Corral, Emily Parry, Julia Cajica, Chung-Mao Pan, Ahmet Kekec, Thomas J. Styers, Christopher Carroll, Rodrigo A. Rodriguez, Kathleen L. McGuire, Stephanie A. Lapera, Joseph D. Brown, Katerina Otrubova
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:5625-5631
We report the synthesis of thirty-six Sansalvamide A derivatives, and their biological activity against colon cancer HT-29 cell line, a microsatellite stable (MSS) colon cancer cell-line. The thirty-six compounds can be divided into three subsets, wh
Autor:
Kai Nakamura, Qiang Li, Tyzoon K. Nomanbhoy, Ann Yu-Jung Shih, Helge Weissig, Oana Cociorva, Lan Pham, John W. Kozarich, Yi Hu, Melissa C. Zhang, Marek Liyanage, Julia Cajica, Kevin R. Shreder, Arwin Aban, Bei Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(18)
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50 = 160 nM) which was co-crystallized with JNK1 to identify key molecular interactio
Autor:
Yi, Hu, Emme C K, Lin, Lan M, Pham, Julia, Cajica, Christopher M, Amantea, Eric, Okerberg, Heidi E, Brown, Allister, Fraser, Lingling, Du, Yasushi, Kohno, Junichi, Ishiyama, John W, Kozarich, Kevin R, Shreder
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(5)
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn(2+)-dependent, 27nM inhibitor of human plasma Lp-PLA(2). Structure-activity relationship studies focused on the AX10479 2-phenylamide gr
Autor:
Kevin R. Shreder, Jonathan S. Rosenblum, Allister Fraser, Ethel McGee, Christopher M. Amantea, Yi Hu, Emme C.K. Lin, Lan M. Pham, John W. Kozarich, Heidi E. Brown, De Michael Chung, Jiangyue Wu, Julia Cajica, Eric Okerberg
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
KIAA1363 is a serine hydrolase whose activity has been shown to be positively associated with tumor cell invasiveness. Thus, inhibitors of KIAA1363 represent a novel targeted therapy approach towards cancer. AX11890 ((1-bromo-2-naphthyl) N,N-dimethyl
Autor:
Kevin R. Shreder, John W. Kozarich, Lingling Du, Emme C.K. Lin, Allister Fraser, Lan Pham, Yasushi Kohno, Jiangyue Wu, Eric Okerberg, Julia Cajica, Yi Hu, Steve J. Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
The hit-to-lead optimization of the HNE inhibitor 5-methyl-2-(2-phenoxy-pyridin-3-yl)-benzo[d][1,3]oxazin-4-one is described. A structure-activity relationship study that focused on the 5 and 7 benzoxazinone positions yielded the optimized 5-ethyl-7-
Autor:
Chung-Mao Pan, Po-Shen Pan, Julia Cajica, Suchitra Ravula, Shelli R. McAlpine, Joseph D. Brown, Thomas J. Styers, Erinprit K. Singh, Emily Parry, Katerina Otrubova, Rodrigo A. Rodriguez, Stephanie A. Lapera
Publikováno v:
The Journal of organic chemistry. 72(6)
We report the synthesis of 34 second-generation Sansalvamide A derivatives. San A derivatives have unique anticancer properties and target multiple cancers, including colon, pancreatic, breast, prostate, and melanoma. As novel templates, the derivati
Autor:
Po-Shen Pan, Ricardo Corral, Irene Medina, Emily Parry, Kristina M. Cook, Julia Cajica, Jennifer V. C. Johnston, Christopher Carroll, Ahmet Kekec, Shelli R. McAlpine, Joseph D. Brown
Publikováno v:
Organic Letters. 7:4785-4785
Described are the syntheses of 14 derivatives of the natural product Sansalvamide A, where two are more active against HCT 116 colon cancer cell lines than the natural product. These derivatives were synthesized using a combinatorial-type strategy th