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 …

[HTML][HTML] Recent advances in the synthesis of di-and trisubstituted hydroxylamines

J Hill, TD Beckler, D Crich - Molecules, 2023 - mdpi.com
As an underrepresented functional group in bioorganic and medicinal chemistry, the
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

BG Cai, Q Li, C Empel, L Li, RM Koenigs, J Xuan - ACS Catalysis, 2022 - ACS Publications
Herein, we report visible light and N-heterocyclic carbene (NHC) jointly promoted
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

L Ripa, J Sandmark, G Hughes… - Journal of Medicinal …, 2023 - ACS Publications
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 …

[HTML][HTML] Discovery of potent pyrrolo-pyrimidine and purine HDAC inhibitors for the treatment of advanced prostate cancer

D Moi, D Bonanni, S Belluti, P Linciano… - European Journal of …, 2023 - Elsevier
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 …

Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer

J Hill, RM Jones, D Crich - Journal of Medicinal Chemistry, 2023 - ACS Publications
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 …

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 …

Chryseochelins—structural characterization of novel citrate-based siderophores produced by plant protecting Chryseobacterium spp.

K Rehm, V Vollenweider, S Gu, VP Friman… - Metallomics, 2023 - academic.oup.com
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 …

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 …

[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 …