The zinc-binding group effect: lessons from non-hydroxamic acid vorinostat analogs
S Geurs, D Clarisse, K De Bosscher… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylases (HDACs) are enzymes pursued as drug targets in various cancers and
several non-oncological conditions, such as inflammation and neurodegenerative disorders …
several non-oncological conditions, such as inflammation and neurodegenerative disorders …
[HTML][HTML] Recent advances in the synthesis of di-and trisubstituted hydroxylamines
As an underrepresented functional group in bioorganic and medicinal chemistry, the
hydroxylamine unit has historically received little attention from the synthetic community …
hydroxylamine unit has historically received little attention from the synthetic community …
Dark and Light Reactions of Carbenes─ Merging Carbene Transfer Reactions with N-Heterocyclic Carbene Catalysis for the Synthesis of Hydroxamic Acid Esters
Herein, we report visible light and N-heterocyclic carbene (NHC) jointly promoted
multicomponent carbene transfer reactions. Under the optimized reaction conditions, two …
multicomponent carbene transfer reactions. Under the optimized reaction conditions, two …
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1, 3, 4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism
Histone deacetylase 6 (HDAC6) is a unique member of the HDAC family mainly targeting
cytosolic nonhistone substrates, such as α-tubulin, cortactin, and heat shock protein 90 to …
cytosolic nonhistone substrates, such as α-tubulin, cortactin, and heat shock protein 90 to …
[HTML][HTML] Discovery of potent pyrrolo-pyrimidine and purine HDAC inhibitors for the treatment of advanced prostate cancer
The development of drugs for the treatment of advanced prostate cancer (PCA) remains a
challenging task. In this study we have designed, synthesized and tested twenty-nine novel …
challenging task. In this study we have designed, synthesized and tested twenty-nine novel …
Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer
Metastases to the brain remain a significant problem in lung cancer, as treatment by most
small-molecule targeted therapies is severely limited by efflux transporters at the blood …
small-molecule targeted therapies is severely limited by efflux transporters at the blood …
A comparative study on the metal complexes of an anticancer estradiol-hydroxamate conjugate and salicylhydroxamic acid
JP Mészáros, H Kovács, G Spengler, F Kovács… - Journal of Inorganic …, 2023 - Elsevier
Hydroxamic acids bearing an (O, O) donor set are well-known metal-chelating compounds
with diverse biological activities including anticancer activity. Since steroid conjugation with …
with diverse biological activities including anticancer activity. Since steroid conjugation with …
Chryseochelins—structural characterization of novel citrate-based siderophores produced by plant protecting Chryseobacterium spp.
Bacteria secrete siderophores whose function is to acquire iron. In recent years, the
siderophores of several Chryseobacterium species were shown to promote the health and …
siderophores of several Chryseobacterium species were shown to promote the health and …
Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors
RF Ahmed, WR Mahmoud, NM Abdelgawad… - European Journal of …, 2023 - Elsevier
This study aimed to design potent carbonic anhydrase inhibitors (CAIs) based on pyrazole
benzenesulfonamide core. Nine series of substituted pyrazole benzenesulfonamide …
benzenesulfonamide core. Nine series of substituted pyrazole benzenesulfonamide …
[HTML][HTML] Using ChEMBL to complement schistosome drug discovery
G Padalino, A Coghlan, G Pagliuca, JE Forde-Thomas… - Pharmaceutics, 2023 - mdpi.com
Schistosomiasis is one of the most important neglected tropical diseases. Until an effective
vaccine is registered for use, the cornerstone of schistosomiasis control remains …
vaccine is registered for use, the cornerstone of schistosomiasis control remains …