Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

SR Alizadeh, SM Hashemi - Medicinal Chemistry Research, 2021 - Springer
Currently, the development of anticancer drug resistance is significantly restricted the clinical
efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely …

New tricks for human farnesyltransferase inhibitor: cancer and beyond

J Wang, X Yao, J Huang - Medchemcomm, 2017 - pubs.rsc.org
Human protein farnesyltransferase (FTase) catalyzes the addition of a C15-farnesyl lipid
group to the cysteine residue located in the COOH-terminal tetrapeptide motif of a variety of …

1, 4-Benzodioxane, an evergreen, versatile scaffold in medicinal chemistry: A review of its recent applications in drug design

C Bolchi, F Bavo, R Appiani, G Roda… - European Journal of …, 2020 - Elsevier
Benzodioxane has long been a versatile template widely employed to design molecules
endowed with diverse bioactivities. Its use spans the last decades of medicinal chemistry …

Benzodioxane–benzamides as new bacterial cell division inhibitors

G Chiodini, M Pallavicini, C Zanotto, M Bissa… - European journal of …, 2015 - Elsevier
A SAR study was performed on 3-substituted 2, 6-difluorobenzamides, known inhibitors of
the essential bacterial cell division protein FtsZ, through a series of modifications first of 2, 6 …

Benzodioxane‐benzamides as antibacterial agents: computational and SAR studies to evaluate the influence of the 7‐substitution in FtsZ interaction

V Straniero, V Sebastián‐Pérez, M Hrast… - …, 2020 - Wiley Online Library
FtsZ is a crucial prokaryotic protein involved in bacterial cell replication. It recently arose as a
promising target in the search for antimicrobial agents able to fight antimicrobial resistance …

Targets and patented drugs for chemotherapy of Chagas disease in the last 15 years-period

V G. Duschak - Recent patents on anti-infective drug discovery, 2016 - benthamdirect.com
Background: The American trypanosomiasis, Chagas disease, is a parasitic infection
typically spread by triatomine vectors affecting millions of people all over Latin America …

New indolizine–chalcones as potent inhibitors of human farnesyltransferase: design, synthesis and biological evaluation

IM Moise, A Ghinet, D Belei, J Dubois, A Farce… - Bioorganic & Medicinal …, 2016 - Elsevier
A new family of indolizine–chalcones was designed, synthesized and screened for the
inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents …

Targeting prenylation inhibition through the mevalonate pathway

P Manaswiyoungkul, ED de Araujo… - RSC Medicinal …, 2020 - pubs.rsc.org
Protein prenylation is a critical mediator in several diseases including cancer and acquired
immunodeficiency syndrome (AIDS). Therapeutic intervention has focused primarily on …

Determinants for α4β2 vs. α3β4 subtype selectivity of pyrrolidine-based nAChRs ligands: A computational perspective with focus on recent cryo-em receptor structures

F Bavo, M Pallavicini, R Appiani, C Bolchi - Molecules, 2021 - mdpi.com
The selectivity of α4β2 nAChR agonists over the α3β4 nicotinic receptor subtype,
predominant in ganglia, primarily conditions their therapeutic range and it is still a complex …

Directed regioselective arylation of imidazo [1, 2-a] pyridine-3-carboxamides using Rh (iii) catalysis

K Jahan, M Sood, O Jain, SC Sahoo… - Organic & Biomolecular …, 2024 - pubs.rsc.org
In contrast to previously reported free-radical pathways to functionalize imidazo [1, 2-a]
pyridines at the C-5 centre, directing group approaches are rare. Herein, we demonstrate a …