Comprehensive review in current developments of benzimidazole‐based medicinal chemistry

RS Keri, A Hiremathad, S Budagumpi… - Chemical biology & …, 2015 - Wiley Online Library
The properties of benzimidazole and its derivatives have been studied over more than one
hundred years. Benzimidazole derivatives are useful intermediates/subunits for the …

[HTML][HTML] Small molecule inhibitors of CXCR4

B Debnath, S Xu, F Grande, A Garofalo, N Neamati - Theranostics, 2013 - ncbi.nlm.nih.gov
CXCR4 is a G-protein-coupled receptor involved in a number of physiological processes in
the hematopoietic and immune systems. The SDF-1/CXCR4 axis is significantly associated …

Entry inhibitors and their use in the treatment of HIV-1 infection

AA Haqqani, JC Tilton - Antiviral research, 2013 - Elsevier
Entry of HIV into target cells is a complex, multi-stage process involving sequential
attachment and CD4 binding, coreceptor binding, and membrane fusion. HIV entry inhibitors …

[HTML][HTML] Benzimidazole: A Versatile Scaffold for Drug Discovery and Beyond-A Comprehensive Review of Synthetic Approaches and Recent Advancements in …

ND Mahurkar, ND Gawhale, MN Lokhande, SJ Uke… - Results in …, 2023 - Elsevier
Heterocyclic compounds are foundational in drug discovery, constituting the core structure of
approximately 80% of pharmaceuticals. Benzimidazole, in particular, emerges as a critical …

Drug discovery research targeting the CXC chemokine receptor 4 (CXCR4)

WT Choi, S Duggineni, Y Xu, Z Huang… - Journal of medicinal …, 2012 - ACS Publications
RECEPTORS Chemokines are small 70 amino acid long soluble proteins that chemoattract
a variety of mononuclear cell types to sites of inflammation or secondary lymphoid organs by …

AMD3100/CXCR4 inhibitor

E De Clercq - Frontiers in immunology, 2015 - frontiersin.org
The original bicyclam, JM1657 (JM standing for Johnson Matthey) was discovered as a
contaminant in a commercial preparation of monocyclams when evaluated for their anti-HIV …

Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists

RK Mishra, AK Shum, LC Platanias, RJ Miller… - Scientific reports, 2016 - nature.com
Abstract The chemokine CXCL12 (SDF-1) and its cognate receptor CXCR4 are involved in a
large number of physiological processes including HIV-1 infectivity, inflammation …

Imaging agents for the chemokine receptor 4 (CXCR4)

J Kuil, T Buckle, FWB van Leeuwen - Chemical Society Reviews, 2012 - pubs.rsc.org
The interaction between the chemokine receptor 4 (CXCR4) and stromal cell-derived factor-
1 (SDF-1, also known as CXCL12) is a natural regulatory process in the human body …

The use of conformational restriction in medicinal chemistry

P de Sena M Pinheiro, DA Rodrigues… - Current topics in …, 2019 - ingentaconnect.com
During the early preclinical phase, from hit identification and optimization to a lead
compound, several medicinal chemistry strategies can be used to improve potency and/or …

Determination of the binding mode for the cyclopentapeptide CXCR 4 antagonist FC 131 using a dual approach of ligand modifications and receptor mutagenesis

S Thiele, J Mungalpara, A Steen… - British Journal of …, 2014 - Wiley Online Library
Background and Purpose The cyclopentapeptide FC 131 (cyclo (‐L‐A rg1‐L‐A rg2‐L‐2‐N
al3‐G ly4‐D‐T yr5‐)) is an antagonist at the CXC chemokine receptor CXCR 4, which plays …