Dihydroorotate dehydrogenase inhibitors in anti-infective drug research

D Boschi, AC Pippione, S Sainas, ML Lolli - European journal of medicinal …, 2019 - Elsevier
Pyrimidines are essential for the cell survival and proliferation of living parasitic organisms,
such as Helicobacter pylori, Plasmodium falciparum and Schistosoma mansoni, that are …

Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold …

S Sainas, M Giorgis, P Circosta… - Journal of Medicinal …, 2021 - ACS Publications
The connection with acute myelogenous leukemia (AML) of dihydroorotate dehydrogenase
(h DHODH), a key enzyme in pyrimidine biosynthesis, has attracted significant interest from …

The synergism between DHODH inhibitors and dipyridamole leads to metabolic lethality in acute myeloid leukemia

V Gaidano, M Houshmand, N Vitale, G Carrà, A Morotti… - Cancers, 2021 - mdpi.com
Simple Summary In this study, we investigated and boosted the pro-apoptotic and pro-
differentiating activity of MEDS433 in acute myeloid leukemia (AML). MEDS433 is an …

Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold …

S Sainas, M Giorgis, P Circosta, G Poli… - Journal of Medicinal …, 2022 - ACS Publications
In recent years, human dihydroorotate dehydrogenase inhibitors have been associated with
acute myelogenous leukemia as well as studied as potent host targeting antivirals. Starting …

Use of the 4-hydroxytriazole moiety as a bioisosteric tool in the development of ionotropic glutamate receptor ligands

S Sainas, P Temperini, JC Farnsworth… - Journal of medicinal …, 2019 - ACS Publications
We report a series of glutamate and aspartate analogues designed using the hydroxy-1, 2, 3-
triazole moiety as a bioisostere for the distal carboxylic acid. Compound 6b showed …

Hydroxyazoles as acid isosteres and their drug design applications—Part 2: Bicyclic systems

AC Pippione, S Sainas, D Boschi, ML Lolli - Advances in Heterocyclic …, 2021 - Elsevier
Hydroxyazoles are acidic systems that are considered isosteres of the carboxylic acid group;
because of their efficacy in exploring chemical space, they are considered an efficient …

Practical Three-Component Regioselective Synthesis of Drug-Like 3-Aryl(or heteroaryl)-5,6-dihydrobenzo[h]cinnolines as Potential Non-Covalent Multi-Targeting …

H Mousavi, M Rimaz, B Zeynizadeh - ACS Chemical …, 2024 - ACS Publications
Neurodegenerative diseases (NDs) are one of the prominent health challenges facing
contemporary society, and many efforts have been made to overcome and (or) control it. In …

Hydroxyazoles as acid isosteres and their drug design applications—Part 1: Monocyclic systems

S Sainas, AC Pippione, D Boschi, ML Lolli - Advances in Heterocyclic …, 2021 - Elsevier
During the optimization process that leads to drug candidates, bioisosterism is often used to
achieve improved potency/selectivity, optimal ADME-T profiles as well as reach intellectual …

Radiosynthesis of [18 F] brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers

VK Banka, S Sainas, E Martino, J Wang… - RSC Medicinal …, 2024 - pubs.rsc.org
Dihydroorotate dehydrogenase (DHODH), an enzyme that plays a critical role in the de novo
pyrimidine biosynthesis, has been recognized as a promising target for the treatment of …

Radiosynthesis of [ 18f]Brequinar for in Vivo PET Imaging of hDHODH in Acute Myeloid Leukemia and Cancers

V Kumar, S Sainas, E Martino, J Wang, ML Lolli… - Available at SSRN … - papers.ssrn.com
Dihydroorotate dehydrogenase (DHODH), an enzyme that plays a critical role in the de-novo
pyrimidine biosynthesis, has been recognized as a promising target for the treatment of …