Results 131 to 140 of about 1,267 (159)

Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2020
The design, synthesis and structure-activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of HIV-1 integrase (ALLINIs) are described. Structural modifications to these molecules were made in order to examine the effect on potency and, for select compounds, pharmacokinetic properties.
Manoj Patel, Christopher Cianci, Christopher W. Allard, Dawn D. Parker, Jean Simmermacher, Susan Jenkins, Brian Mcauliffe, Beatrice Minassian, Linda Discotto, Mark Krystal, Nicholas A. Meanwell, B. Narasimhulu Naidu   +11 more
openaire   +2 more sources

Discovery of a Distinct Chemical and Mechanistic Class of Allosteric HIV-1 Integrase Inhibitors with Antiretroviral Activity

ACS Chemical Biology, 2017
Allosteric integrase inhibitors (ALLINIs) bind to the lens epithelial-derived growth factor (LEDGF) pocket on HIV-1 integrase (IN) and possess potent antiviral effects. Rather than blocking proviral integration, ALLINIs trigger IN conformational changes that have catastrophic effects on viral maturation, rendering the virions assembled in the presence ...
Christine Burlein, Cheng Wang, Min Xu, Triveni Bhatt, Mark Stahlhut, Yangsi Ou, Gregory C. Adam, Jeffrey Heath, Daniel J. Klein, John Sanders, Kartik Narayan, Pravien Abeywickrema, Mee Ra Heo, Steven S. Carroll, Jay A. Grobler, Sujata Sharma, Tracy L. Diamond, Antonella Converso, Daniel J. Krosky   +18 more
openaire   +2 more sources

Crystal Structures of Novel Allosteric Peptide Inhibitors of HIV Integrase Identify New Interactions at the LEDGF Binding Site

ChemBioChem, 2011
AbstractAn optimised method of solution cyclisation gave us access to a series of peptides including SLKIDNLD (2). We investigated the crystallographic complexes of the HIV integrase (HIV‐IN) catalytic core domain with 13 of the peptides and identified multiple interactions at the binding site, including hydrogen bonds with residues Thr125 and Gln95 ...
David I, Rhodes, Thomas S, Peat, Nick, Vandegraaff, Dharshini, Jeevarajah, Janet, Newman, John, Martyn, Jonathan A V, Coates, Nicholas J, Ede, Philip, Rea, John J, Deadman   +9 more
openaire   +2 more sources

Expeditious Synthesis of a Potent Allosteric HIV-1 Integrase Inhibitor GSK3839919A

Organic Process Research & Development, 2023
Mark A. Bobko, Jennifer M. Elward, B. Narasimhulu Naidu, Yexenia E. Nieves-Quinones, Christopher A. Reiher, Qiaogong Su, Liang Sun, John Woodard, Shiping Xie, Wuxing Yang, Yunxing Yin   +10 more
openaire   +1 more source

Design and synthesis of novel and potent allosteric HIV-1 integrase inhibitors with a spirocyclic moiety

Bioorganic & Medicinal Chemistry Letters
We report herein the design and discovery of novel allosteric HIV-1 integrase inhibitors. Our design concept utilized the spirocyclic moiety to restrain the flexibility of the conformation of the lipophilic part of the inhibitor. Compound 5 showed antiviral activity by binding to the nuclear lens epithelium-derived growth factor (LEDGF/p75) binding ...
Kaoru, Adachi, Tomoyuki, Manabe, Takayuki, Yamasaki, Akira, Suma, Takuya, Orita, Tomoko, Furuzono, Tsuyoshi, Adachi, Yoshitsugu, Ohata, Yoshiyuki, Akiyama, Susumu, Miyazaki   +9 more
openaire   +2 more sources

A Potent Allosteric Inhibitor of HIV-1 Integrase

Synfacts, 2022
openaire   +1 more source

The Development of HIV-1 Integrase Allosteric Inhibitors Using a Fragment Based Drug Discovery Approach

2018
HIV-1 integrase (IN) is an enzyme that is essential for viral replication. Previous work within our group identified a molecule as a hit that bound to IN and had potential to be developed as an inhibitor of HIV. This thesis describes the hit-to-lead optimisation process of developing the hit into a high-affinity lead compound using a Fragment-Based ...
openaire   +1 more source

Synthesis of an Allosteric HIV-1 Integrase Inhibitor

Synfacts, 2020
openaire   +1 more source

The broadening scope of oral mucositis and oral ulcerative mucosal toxicities of anticancer therapies

Ca-A Cancer Journal for Clinicians, 2022
Sharon Elad, Noam Yarom, Yehuda Zadik
exaly  

Allosteric Integrase Inhibitors

2016
Victoria Hann, Peter Dawson, Mark Ashton
openaire   +1 more source