Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Virginia Schwinge"'
Autor:
Louis M. Renzetti, Li Chen, Karen Rowan, Allen Sheffron, Tai-Nan Huang, Jian Ping Lou, Jefferson Wright Tilley, Kenneth G. Hull, Virginia Schwinge, Gerry Kaplan, Achyutharao Sidduri, Robert M. Campbell, Robert William Guthrie, Nicholas John Silvester Huby
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2475-2478
A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53da7a5e27aecfcea2db394b82b8d572
https://doi.org/10.1016/s0960-894x(02)00386-4
https://doi.org/10.1016/s0960-894x(02)00386-4
Autor:
Karen Rowan, Jian Ping Lou, Tai-Nan Huang, Gerry Kaplan, Jefferson Wright Tilley, Achyutharao Sidduri, Robert M. Campbell, Virginia Schwinge, Robert William Guthrie, Louis M. Renzetti, Li Chen, Frank Mennona
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2479-2482
A series of N-benzoyl-4-[(2,6-dichlorobenzoyl)amino]-L-phenylalanine derivatives was prepared in order to optimize the substitution on the N-benzoyl moiety for VCAM/VLA-4 antagonist activity. Disubstitution in the 2- and 6-positions is favored and a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7773fe43cdcb34c6ef40df81c00af4b1
https://doi.org/10.1016/s0960-894x(02)00387-6
https://doi.org/10.1016/s0960-894x(02)00387-6
Autor:
Karen Rowan, Jefferson Wright Tilley, Richard V. Trilles, Dorota Miklowski, Virginia Schwinge, Li Chen, Tai-Nan Huang, Robert M. Campbell, David C. Fry
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1679-1682
A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afd7d731fdb244de48ba4c2810efc9ab
https://doi.org/10.1016/s0960-894x(02)00201-9
https://doi.org/10.1016/s0960-894x(02)00201-9
Autor:
Li Chen, Weiya Yun, Richard V. Trilles, Karen Rowan, David C. Fry, Jefferson Wright Tilley, Charles H. Cook, Virginia Schwinge, Robert M. Campbell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:137-140
A series of N-benzylpyroglutamyl-L-phenylalanine derivatives bearing carbamoyl substituents in the 3- or 4-positions was prepared and assayed for inhibition of the interaction between VCAM and VLA-4. Potent inhibition was observed in a number of anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e28b1c8519567294c5c8237e485742d
https://doi.org/10.1016/s0960-894x(01)00711-9
https://doi.org/10.1016/s0960-894x(01)00711-9
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1-4
A series of imides and lactams derived from 4-amino-N-benzylpyroglutamyl- l -phenylalanine was prepared and evaluated for activity as VCAM/VLA-4 antagonists. Imides were more potent than the corresponding lactams; several had subnanomolar IC50s in an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e29778b91f08dd46a7eeb83de7bcd0c5
https://doi.org/10.1016/s0960-894x(00)00582-5
https://doi.org/10.1016/s0960-894x(00)00582-5
Autor:
Dorota Miklowski, Richard V. Trilles, Robert William Guthrie, Karen Rowan, Gerry Kaplan, Nicolas Huby, Barry A. Wolitzky, Jefferson Wright Tilley, Virginia Schwinge, Francis A. Mennona, Tai-Nan Huang, Li Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:729-733
A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d9701ff0e4ce4f658c7cfcb49aaa55f
https://doi.org/10.1016/s0960-894x(00)00089-5
https://doi.org/10.1016/s0960-894x(00)00089-5
Autor:
Richard V. Trilles, David C. Fry, Virginia Schwinge, Weiya Yun, Robert M. Campbell, Karen Rowan, Li Chen, Charles H. Cook, Jefferson Wright Tilley
Publikováno v:
ChemInform. 33
A series of N-benzylpyroglutamyl-L-phenylalanine derivatives bearing carbamoyl substituents in the 3- or 4-positions was prepared and assayed for inhibition of the interaction between VCAM and VLA-4. Potent inhibition was observed in a number of anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b6227c1cfc9d5e9c0042ad46a477247b
https://doi.org/10.1002/chin.200219183
https://doi.org/10.1002/chin.200219183
Autor:
Pramod Joshi, Angela Hanglow, Karen Rowan, Jefferson Wright Tilley, Charles M. Cook, Gerry Kaplan, Barry A. Wolitzky, Nader Fotouhi, David C. Fry, Virginia Schwinge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1171-1173
The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95eeb8bf78bfdbddf88b03b36317d223
https://doi.org/10.1016/s0960-894x(00)00174-8
https://doi.org/10.1016/s0960-894x(00)00174-8
Autor:
Barry A. Wolitzky, Virginia Schwinge, Karen Rowan, Pramod Joshi, Jefferson Wright Tilley, Nader Fotouhi
Publikováno v:
ChemInform. 31
Selective substitution of a sulfur atom by carbon in a highly potent 13-membered cyclic disulfide was accomplished by intramolecular displacement of a bromide. The potency of the resulting thioethers in the VCAM/VLA-4 assay was dependant on ring size
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ead0d1bfcea91bb1de946b709b590a60
https://doi.org/10.1002/chin.200039150
https://doi.org/10.1002/chin.200039150
Autor:
Virginia Schwinge, Karen Rowan, Jefferson Wright Tilley, Nader Fotouhi, Pramod Joshi, Barry A. Wolitzky
Publikováno v:
Bioorganicmedicinal chemistry letters. 10(11)
Selective substitution of a sulfur atom by carbon in a highly potent 13-membered cyclic disulfide was accomplished by intramolecular displacement of a bromide. The potency of the resulting thioethers in the VCAM/VLA-4 assay was dependant on ring size
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b5415fef5b2fd46f7002a192cc0e21b
https://pubmed.ncbi.nlm.nih.gov/10866373
https://pubmed.ncbi.nlm.nih.gov/10866373