Triazoles in medicinal chemistry: physicochemical properties, bioisosterism, and application

Q Guan, S **ng, L Wang, J Zhu, C Guo… - Journal of Medicinal …, 2024 - ACS Publications
Triazole demonstrates distinctive physicochemical properties, characterized by weak
basicity, various dipole moments, and significant dual hydrogen bond acceptor and donor …

Aldo-keto reductases and cancer drug resistance

TM Penning, S Jonnalagadda, PC Trippier… - Pharmacological …, 2021 - Elsevier
Human aldo-keto reductases (AKRs) catalyze the NADPH-dependent reduction of carbonyl
groups to alcohols for conjugation reactions to proceed. They are implicated in resistance to …

Overview of AKR1C3: inhibitor achievements and disease insights

Y Liu, S He, Y Chen, Y Liu, F Feng, W Liu… - Journal of medicinal …, 2020 - ACS Publications
Human aldo-keto reductase family 1 member C3 (AKR1C3) is known as a hormone activity
regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone …

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 …

The role of adrenal derived androgens in castration resistant prostate cancer

M Barnard, EA Mostaghel, RJ Auchus… - The Journal of steroid …, 2020 - Elsevier
Castration resistant prostate cancer (CRPC) remains androgen dependant despite castrate
levels of circulating testosterone following androgen deprivation therapy, the first line of …

AKR1C3 in carcinomas: From multifaceted roles to therapeutic strategies

M Li, L Zhang, J Yu, X Wang, L Cheng, Z Ma… - Frontiers in …, 2024 - frontiersin.org
Aldo-Keto Reductase Family 1 Member C3 (AKR1C3), also known as type 5 17β-
hydroxysteroid dehydrogenase (17β-HSD5) or prostaglandin F (PGF) synthase, functions as …

Use of human dihydroorotate dehydrogenase (hDHODH) inhibitors in autoimmune diseases and new perspectives in cancer therapy

ML Lolli, S Sainas, AC Pippione… - Recent Patents on …, 2018 - benthamdirect.com
Background: Human dihydroorotate dehydrogenase (hDHODH, EC 1.3. 5.2), a
flavindependent mitochondrial enzyme involved in de novo pyrimidine biosynthesis, is a …

Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors

S Sainas, AC Pippione, E Lupino… - Journal of medicinal …, 2018 - ACS Publications
Human dihydroorotate dehydrogenase (h DHODH) catalyzes the rate-limiting step in de
novo pyrimidine biosynthesis, the conversion of dihydroorotate to orotate. h DHODH has …

Development of novel AKR1C3 inhibitors as new potential treatment for castration-resistant prostate cancer

S Endo, H Oguri, J Segawa, M Kawai… - Journal of medicinal …, 2020 - ACS Publications
Aldo–keto reductase (AKR) 1C3 catalyzes the synthesis of active androgens that promote
the progression of prostate cancer. AKR1C3 also contributes to androgen-independent cell …

Fenamates: Forgotten treasure for cancer treatment and prevention: Mechanisms of action, structural modification, and bright future

J Li, X Wang, H Zhang, X Hu, X Peng… - Medicinal Research …, 2025 - Wiley Online Library
Fenamates as classical nonsteroidal anti‐inflammatory agents are widely used for relieving
pain. Preclinical studies and epidemiological data highlight their chemo‐preventive and …