Tricyclic HIV integrase inhibitors: Potent and orally bioavailable C5-aza analogs

被引：19

作者：

Jin, Haolun ^{[1
]}

Wright, Matthew ^{[1
]}

Pastor, Richard ^{[1
]}

Mish, Michael ^{[1
]}

Metobo, Sammy ^{[1
]}

Jabri, Salman ^{[1
]}

Lansdown, Rachael ^{[1
]}

Cai, Ruby ^{[1
]}

Pyun, Peter ^{[1
]}

Tsiang, Manuel ^{[1
]}

Chen, Xiaowu ^{[1
]}

Kim, Choung U. ^{[1
]}

机构：

[1] Gilead Sci Inc, Dept Med Chem, Foster City, CA 94404 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 04期

关键词：

D O I：

10.1016/j.bmcl.2008.01.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound ( compound 9) was identified and selected for development. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1388 / 1391

页数：4

共 50 条

[21] Optimization of a series of potent, selective and orally bioavailable SYK inhibitors
Grimster, Neil P.
Gingipalli, Lakshmaiah
Barlaam, Bernard
Su, Qibin
Zheng, XiaoLan
Watson, David
Wang, Haixia
Simpson, Iain
Pike, Andy
Balazs, Amber
Boiko, Scott
Ikeda, Timothy P.
Impastato, Anna C.
Jones, Natalie H.
Kawatkar, Sameer
Kemmitt, Paul
Lamont, Scott
Patel, Joe
Read, Jon
Sarkar, Ujjal
Sha, Li
Tomlinson, Ronald C.
Wang, Haiyun
Wilson, David M.
Zehnder, Troy E.
Wang, Lianghe
Wang, Peng
Goldberg, Frederick W.
Shao, Wenlin
Fawell, Stephen
Dry, Hannah
Dowling, James E.
Edmondson, Scott D.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 30 (19)
[22] Design and Optimization of Potent and Orally Bioavailable Tetrahydronaphthalene Raf Inhibitors
Gould, Alexandra E.
Adams, Ruth
Adhikari, Sharmila
Aertgeerts, Kathleen
Afroze, Roushan
Blackburn, Christopher
Calderwood, Emily F.
Chau, Ryan
Chouitar, Jouhara
Duffey, Matthew O.
England, Dylan B.
Farrer, Cheryl
Forsyth, Nancy
Garcia, Khristofer
Gaulin, Jeffery
Greenspan, Paul D.
Guo, Ribo
Harrison, Sean J.
Huan, Shih-Chung
Iartchouk, Natalia
Janowick, Dave
Kim, Mi-Sook
Kulkarni, Bheemashankar
Langston, Steven P.
Liu, Jane X.
Ma, Li-Ting
Menon, Saurabh
Mizutani, Hirotake
Paske, Erin
Renou, Christelle C.
Rezaei, Mansoureh
Rowland, R. Scott
Sintchak, Michael D.
Smith, Michael D.
Stroud, Stephen G.
Tregay, Ming
Tian, Yuan
Veiby, Ole P.
Vos, Tricia J.
Vyskocil, Stepan
Williams, Juliet
Xu, Tianlin
Yang, Johnny J.
Yano, Jason
Zeng, Hongbo
Zhang, Dong Mei
Zhang, Qin
Galvin, Katherine M.
JOURNAL OF MEDICINAL CHEMISTRY, 2011, 54 (06) : 1836 - 1846
[23] A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors
Tucker, Thomas J.
Embrey, Mark W.
Alleyne, Candice
Amin, Rupesh P.
Bass, Alan
Bhatt, Bhavana
Bianchi, Elisabetta
Branca, Danila
Bueters, Tjerk
Buist, Nicole
Ha, Sookhee N.
Hafey, Mike
He, Huaibing
Higgins, John
Johns, Douglas G.
Kerekes, Angela D.
Koeplinger, Kenneth A.
Kuethe, Jeffrey T.
Li, Nianyu
Murphy, BethAnn
Orth, Peter
Salowe, Scott
Shahripour, Aurash
Tracy, Rodger
Wang, Weixun
Wu, Chengwei
Xiong, Yusheng
Zokian, Hratch J.
Wood, Harold B.
Walji, Abbas
JOURNAL OF MEDICINAL CHEMISTRY, 2021, 64 (22) : 16770 - 16800
[24] A potent and orally active HIV-1 integrase inhibitor
Egbertson, Melissa S.
Moritz, H. Marie
Melamed, Jeffrey Y.
Han, Wei
Perlow, Debra S.
Kuo, Michelle S.
Embrey, Mark
Vacca, Joseph P.
Zrada, Matthew M.
Cortes, Amanda R.
Wallace, Audrey
Leonard, Yvonne
Hazuda, Daria J.
Miller, Michael D.
Felock, Peter J.
Stillmock, Kara A.
Witmer, Marc V.
Schleif, William
Gabryelski, Lori J.
Moyer, Gregory
Ellis, Joan D.
Jin, Lixia
Xu, Wei
Braun, Matthew P.
Kassahun, Kellem
Tsou, Nancy N.
Young, Steven D.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (05) : 1392 - 1398
[25] Indole Derivatives Are Potent Inhibitors of HIV Integrase
Selvam, Periyasamy
Maddali, Kasthuraiah
Pommier, Yves
ANTIVIRAL RESEARCH, 2009, 82 (02) : A42 - A42
[26] From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors
Liang, Jun
Labadie, Sharada
Zhang, Birong
Ortwine, Daniel F.
Patel, Snahel
Vinogradova, Maia
Kiefer, James R.
Mauer, Till
Gehling, Victor S.
Harmange, Jean-Christophe
Cummings, Richard
Lai, Tommy
Liao, Jiangpeng
Zheng, Xiaoping
Liu, Yichin
Gustafson, Amy
Van der Porten, Erica
Mao, Weifeng
Liederer, Bianca M.
Deshmukh, Gauri
An, Le
Ran, Yingqing
Classon, Marie
Trojer, Patrick
Dragovich, Peter S.
Murray, Lesley
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (13) : 2974 - 2981
[27] Solid Phase Synthesis of Novel Pyrrolidinedione Analogs as Potent HIV-1 Integrase Inhibitors
Pendri, Annapurna
Troyer, Timothy L.
Sofia, Michael J.
Walker, Michael A.
Naidu, B. Narasimhulu
Banville, Jacques
Meanwell, Nicholas A.
Dicker, Ira
Lin, Zeyu
Krystal, Mark
Gerritz, Samuel W.
JOURNAL OF COMBINATORIAL CHEMISTRY, 2010, 12 (01): : 84 - 90
[28] Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT
Parthasarathy, Saravanan
Henry, Kenneth
Pei, Huaxing
Clayton, Josh
Rempala, Mark
Johns, Deidre
De Frutos, Oscar
Garcia, Pablo
Mateos, Carlos
Pleite, Sehila
Wang, Yong
Stout, Stephanie
Condon, Bradley
Ashok, Sheela
Lu, Zhohai
Ehlhardt, William
Raub, Tom
Lai, Mei
Geeganage, Sandaruwan
Burkholder, Timothy P.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (10) : 1887 - 1891
[29] Identification of potent, orally bioavailable nonnucleoside HCV RNA polymerase inhibitors
Dragovich, Peter S.
Brooks, Jennifer
Bartkowski, Darian M.
Blazel, Julie K.
Dao, Kimkim
Ellis, David A.
Gobbi, Alberto
Kamran, Ruhi
Kim, Sun Hee
LeBrun, Laurie A.
Li, Lian-Sheng
Murphy, Douglas E.
Nolan, Thomas G.
Norris, Daniel A.
Patel, Rupal
Ruebsam, Frank
Sergeeva, Maria V.
Shah, Amit M.
Showalter, Richard E.
Stankovic, Nebojsa
Sun, Zhongxiang
Tran, Chinh V.
Tran, Martin T.
Tsan, Mei
Webber, Stephen E.
Xiang, Alan X.
Zhao, Jingjing
Kirkovsky, Leo
Zhou, Yuefen
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 237
[30] Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors
Garton, Neil S.
Barker, Michael D.
Davis, Rob P.
Douault, Clement
Hooper-Greenhill, Edward
Jones, Emma
Lewis, Huw D.
Liddle, John
Lugo, Dave
McCleary, Scott
Preston, Alex G. S.
Ramirez-Molina, Cesar
Neu, Margarete
Shipley, Tracy J.
Somers, Don O.
Watson, Robert J.
Wilson, David M.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (19) : 4606 - 4612

← 1 2 3 4 5 →