HIV-1 integrase strand transfer inhibitors (INSTIs): Design, synthesis and biological activity

被引：0

作者：

Ferro, S. ^{[1
]}

Barreca, M. L. ^{[1
]}

De Luca, L. ^{[1
]}

Rao, A. ^{[1
]}

Monforte, A. M. ^{[1
]}

Michiels, M.

Witvrouw, M.

Debyser, Z.

Chimirri, A. ^{[1
]}

机构：

[1] Univ Messina, Dip Farmacochim, I-98168 Messina, Italy

来源：

PROCEEDINGS OF THE 5TH JOINT MEETING ON MEDICINAL CHEMISTRY | 2007年

关键词：

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In recent years a 3D-pharmacophore model has allowed us to rationally design potent INSTIs. On this basis we synthesized a series of new benzylindole derivatives through efficient solution-phase parallel and microwave-assisted syntheses. Biological evaluation of compounds obtained pointed to a potent IN strand-transfer inhibitory activity.

引用

页码：11 / 15

页数：5

共 50 条

[31] Optimization of the benzyl moiety in 2-pyridone aminals as HIV integrase strand transfer inhibitors (InSTIs)
Ferguson, Ron
Yu, Tao
Zhang, Yonglian
Graham, Thomas
Liu, Wensheng
Waddell, Sherman
Stamford, Andrew
Walji, Abbas
Raheem, Izzat
Wai, John
Coleman, Paul
Verras, Andreas
Sanders, John
Xu, Min
Grobler, Jay
Schreier, John
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2019, 258
[32] Design, synthesis, and biological evaluation of chicoric acid analogs as inhibitors of HIV-1 integrase
Charvat, Trevor T.
Lee, Deborah J.
Robinson, W. Edward
Chamberlin, A. Richard
BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (13) : 4552 - 4567
[33] Design, Synthesis, and Biological Evaluation of 1,2-Dihydroisoquinolines as HIV-1 Integrase Inhibitors
Tandon, Vibha
Urvashi
Yaday, Pooja
Sur, Souvik
Abbat, Sheenu
Tiwari, Vinod
Hewer, Raymond
Papathanasopoulos, Maria A.
Raja, Rameez
Banerjea, Akhil C.
Verma, Akhilesh K.
Kukreti, Shrikant
Bharatam, Prasad V.
ACS MEDICINAL CHEMISTRY LETTERS, 2015, 6 (10): : 1065 - 1070
[34] A Practical Approach to Bicyclic Carbamoyl Pyridones with Application to the Synthesis of HIV-1 Integrase Strand Transfer Inhibitors
Mahajan, Pankaj S.
Smith, Steven J.
Hughes, Stephen H.
Zhao, Xuezhi
Burke, Terrence R., Jr.
MOLECULES, 2023, 28 (03):
[35] Impact of combinations of clinically observed HIV integrase mutations on phenotypic resistance to integrase strand transfer inhibitors (INSTIs): a molecular study
Cheung, Peter K.
Shahid, Aniqa
Dong, Winnie
Lepik, Katherine J.
Montaner, Julio S. G.
Brockman, Mark A.
Brumme, Zabrina L.
Brumme, Chanson J.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2022, 77 (04) : 979 - 988
[36] De novo design and synthesis of HIV-1 integrase inhibitors
Makhija, MT
Kasliwal, RT
Kulkarni, VM
Neamati, N
BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (09) : 2317 - 2333
[37] Structural effects of HIV-1 subtype C integrase mutations on the activity of integrase strand transfer inhibitors in South African patients
Mbhele, Nokuzola
Gordon, Michelle
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2022, 40 (23): : 12546 - 12556
[38] Susceptibility to HIV-1 integrase strand transfer inhibitors (INSTIs) in highly treatment-experienced patients who failed an INSTI-based regimen
Santoro, Maria M.
Fornabaio, Chiara
Malena, Marina
Galli, Laura
Poli, Andrea
Menozzi, Marianna
Zazzi, Maurizio
White, Kirsten L.
Castagna, Antonella
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2020, 56 (01)
[39] Surface plasmon resonance study on HIV-1 integrase strand transfer activity
Hana Vaisocherová
Jan Snášel
Tomáš Špringer
Hana Šípová
Ivan Rosenberg
Josef Štěpánek
Jiří Homola
Analytical and Bioanalytical Chemistry, 2009, 393 : 1165 - 1172
[40] Surface plasmon resonance study on HIV-1 integrase strand transfer activity
Vaisocherova, Hana
Snasel, Jan
Springer, Tomas
Sipova, Hana
Rosenberg, Ivan
Stepanek, Josef
Homola, Jiri
ANALYTICAL AND BIOANALYTICAL CHEMISTRY, 2009, 393 (04) : 1165 - 1172

← 1 2 3 4 5 →