An appraisal of anticancer activity with structure–activity relationship of quinazoline and quinazolinone analogues through EGFR and VEGFR inhibition: A review

K Haider, S Das, A Joseph… - Drug Development …, 2022 - Wiley Online Library
Cancer is one of the leading causes of death. Globally a huge number of deaths and new
incidences are reported annually. Heterocyclic compounds have been proved to be very …

Current perspectives on quinazolines with potent biological activities: A review

T Gupta, A Rohilla, A Pathak, MJ Akhtar… - Synthetic …, 2018 - Taylor & Francis
Quinazoline is a heterocyclic compound having biological activities. It is aromatic in nature
having bicyclic structure containing benzene ring and pyrimidine ring. Quinazoline and its …

S-Alkylated quinazolin-4 (3 H)-ones as dual EGFR/VEGFR-2 kinases inhibitors: design, synthesis, anticancer evaluation and docking study

SS Tawfik, A Hamdi, AR Ali, AA Elgazar… - RSC …, 2024 - pubs.rsc.org
Dual targeting by a single molecule has emerged as a promising strategy for fighting cancer.
In this study, a new set of 2-thioquinazolin-4 (3H)-ones as potential anti-cancer surrogates …

Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors

E Barbosa da Silva, DA Rocha, IS Fortes… - Journal of Medicinal …, 2021 - ACS Publications
The cysteine proteases, cruzain and Tbr CATL (rhodesain), are therapeutic targets for
Chagas disease and Human African Trypanosomiasis, respectively. Among the known …

A quinquennial review on recent advancements and developments in search of anti-malarial agents

TM Dhameliya, D Kathuria, TM Patel… - Current Topics in …, 2023 - benthamdirect.com
Malaria has been a major parasitic disease in tropical and subtropical regions and is
estimated to kill between one and two million people (mainly children) every year. Novel anti …

[HTML][HTML] Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3

PPS Calic, TD Ashton, M Mansouri, K Loi… - European Journal of …, 2024 - Elsevier
Emerging resistance to current antimalarials is reducing their effectiveness and therefore
there is a need to develop new antimalarial therapies. Toward this goal, high throughput …

Property and activity refinement of dihydroquinazolinone-3-carboxamides as orally efficacious antimalarials that target PfATP4

TD Ashton, PPS Calic, MG Dans, ZK Ooi… - Journal of Medicinal …, 2024 - ACS Publications
To contribute to the global effort to develop new antimalarial therapies, we previously
disclosed initial findings on the optimization of the dihydroquinazolinone-3-carboxamide …

Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease

CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …

Chemo‐proteomics in antimalarial target identification and engagement

BL Bailey, W Nguyen, AF Cowman… - Medicinal Research …, 2023 - Wiley Online Library
Humans have lived in tenuous battle with malaria over millennia. Today, while much of the
world is free of the disease, areas of South America, Asia, and Africa still wage this war with …

Optimization of 2, 3-dihydroquinazolinone-3-carboxamides as antimalarials targeting PfATP4

TD Ashton, MG Dans, P Favuzza, A Ngo… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need to populate the antimalarial clinical portfolio with new candidates
because of resistance against frontline antimalarials. To discover new antimalarial …