Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Dauphine Barone"'
Autor:
J.S. Skotnicki, James M. Chen, Jun Xu, Dauphine Barone, L.M. Laakso, J. Schmid, Weixin Xu, G. Jin, Terri Cummons, Jeremy I. Levin, Mila T. Du
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1605-1609
A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1′ groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a mode
Autor:
Arie Zask, Xuemei Du, Jeremy I. Levin, Terri Cummons, Semiramis Ayral-Kaloustian, Jerauld S. Skotnicki, Gloria Jean Macewan, Dauphine Barone, Nancy H. Eudy, Vincent Sandanayaka, Guixian Jin, Jun Xu, Joshua Kaplan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1641-1645
Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-α release. Oral activity in the mouse LPS model of TNF-α r
Autor:
Gloria Jean Macewan, Semiramis Ayral-Kaloustian, Terri Cummons, James M. Chen, Frances C. Nelson, Jun Xu, Dauphine Barone, Efren Guillermo Delos Santos, Mila T. Du, Jeremy I. Levin, Guixian Jin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4147-4151
A series of benzodiazepine MMP/TACE inhibitors bearing polar moieties has been synthesized in an effort to optimize inhibitory activity against LPS-stimulated TNF production in human monocytes and oral activity in a murine LPS model.
Autor:
Aranapakam Mudumbai Venkatesan, Amy Sung, John W. Ellingboe, Diane Joseph Mccarthy, Jerauld S. Skotnicki, Jamie Marie Davis, Jannie Lea Baker, Weixin Xu, Arie Zask, Dauphine Barone, G. Jin, John F. DiJoseph, Levin Jeremy Ian, George Theodore Grosu
Publikováno v:
Journal of medicinal chemistry. 47(25)
A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized. Their structure-activity relationships, against tumor necrosis factor-alpha (TACE) and matrix metalloproteinase (MMP)
Autor:
Gloria Jean Macewan, Chuansheng Niu, J.S. Skotnicki, Dauphine Barone, A. Zask, C. Crago, Ayral-Kaloustian Semiranis, Amy Sung, Roy A. Black, R. Cowling, Kendall M. Mohler, Terri Cummons, Gulnaz Khafizova, Jeremy I. Levin, Derek C. Cole, E. Delos Santos, E.J. Salaski, Katherine Cheung, G. Jin, Yuhua Zhang, Weixin Xu, X. Du, James M. Chen, Jun Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(16)
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, all bearing a butynyloxy P1' group, was explored. In particular, compound 5j has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1
Autor:
Loran M. Killar, S. Skala, James M. Chen, X. Du, G. Jin, Roy A. Black, A. Zask, Michele A. Sharr, Gu Yansong, R. Cowling, C.J March, J.S. Skotnicki, J. D. Albright, Amy Sung, Dauphine Barone, John F. DiJoseph, C. E. Roth, Kendall M. Mohler, Jeremy I. Levin, M. Hogan
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(8)
Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by varia
Autor:
Terri Cummons, X. Du, James M. Chen, Dauphine Barone, E. Delos Santos, Amy Sung, G. Jin, Jun Xu, R. Cowling, Jay D. Albright, Mila T. Du, R. Mulvey, Frances C. Nelson, S. Skala, Roy A. Black, J.S. Skotnicki, Jeremy I. Levin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::359c750cebb10f7dfdca1ec34e96a6db
https://doi.org/10.1016/b978-0-08-044304-1.50138-6
https://doi.org/10.1016/b978-0-08-044304-1.50138-6
Publikováno v:
Toxicologic pathology. 30(3)
Periosteal hyperostosis (exostosis) was identified in 5.9% (11/188) of DBA/1 male mice 10—14 weeks old used for collagen-induced arthritis (CIA) efficacy testing of immunomodulatory biologics. Mice with and without CIA in the affected limb, and als
Autor:
R. Cowling, Amy Sung, C.J March, Jeremy I. Levin, Roy A. Black, G. Jin, Frances C. Nelson, S. Skala, Dauphine Barone, James M. Chen, Kendall M. Mohler, Loran M. Killar, Mila T. Du, J.S. Skotnicki
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(8)
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1′ groups was explored. In particular, compound 4t bearing a butynyloxy P1′ moiety has excellent in vitro potency against isolated TACE enzyme and in
Autor:
Yuhua, Zhang, Jun, Xu, Jeremy, Levin, Martin, Hegen, Guangde, Li, Heidi, Robertshaw, Fionula, Brennan, Terri, Cummons, Dave, Clarke, Nichole, Vansell, Cheryl, Nickerson-Nutter, Dauphine, Barone, Ken, Mohler, Roy, Black, Jerry, Skotnicki, Jay, Gibbons, Marc, Feldmann, Philip, Frost, Glenn, Larsen, Lih-Ling, Lin
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics; April 2004, Vol. 309 Issue: 1 p348-55, 8p