Regulation of biological processes by intrinsically chiral engineered materials

B Ma, A Bianco - Nature Reviews Materials, 2023 - nature.com
Chirality has a key role in the synthesis of biomolecules and the development of life.
Although the effects of many chiral molecules or materials on biological processes have …

Recent advances in urea-and thiourea-containing compounds: focus on innovative approaches in medicinal chemistry and organic synthesis

R Ronchetti, G Moroni, A Carotti, A Gioiello… - RSC Medicinal …, 2021 - pubs.rsc.org
Urea and thiourea represent privileged structures in medicinal chemistry. Indeed, these
moieties constitute a common framework of a variety of drugs and bioactive compounds …

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 …

Carboxylic acid bioisosteres in medicinal chemistry: synthesis and properties

K Bredael, S Geurs, D Clarisse… - Journal of …, 2022 - Wiley Online Library
Lead optimization represents the tedious process of fine‐tuning lead compounds from
biologically active hits to suitable drug candidates for clinical trials. By chemically modifying …

Squaric acid-based radiopharmaceuticals for tumor imaging and therapy

T Grus, H Lahnif, B Klasen, ES Moon… - Bioconjugate …, 2021 - ACS Publications
Targeting vectors bound to a chelator represent a significant fraction of
radiopharmaceuticals used nowadays for diagnostic and therapeutic purposes in nuclear …

Squaramide-tethered sulfonamides and coumarins: Synthesis, inhibition of tumor-associated CAs IX and XII and docking simulations

G Arrighi, A Puerta, A Petrini, FJ Hicke… - International Journal of …, 2022 - mdpi.com
(1) Background: carbonic anhydrases (CAs) are attractive targets for the development of
new anticancer therapies; in particular, CAs IX and XII isoforms are overexpressed in …

Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors

L Yan, Q Wang, L Liu, Y Le - Journal of Enzyme Inhibition and …, 2022 - Taylor & Francis
This paper described our efforts to develop dianilinopyrimidines as novel EGFR inhibitors.
All the target compounds were tested for inhibitory effects against wild type EGFR (EGFRwt) …

Palladium-catalyzed domino reaction for the assembly of norbornane-containing chromones with dimethyl squarate as the solid C1 source

F Li, HM Li, RF Xiu, JK Zhang, BD Cui, NW Wan… - Organic …, 2022 - ACS Publications
Reported herein is a novel palladium-catalyzed [2+ 2+ 1] domino annulation of 3-
iodochromones, bridged olefins, and dimethyl squarate allowing the construction of …

Direct gem‐Difluoroalkenylation of X−H Bonds with Trifluoromethyl Ketone N‐Triftosylhydrazones for Synthesis of Tetrasubstituted Heteroatomic gem …

X Zhang, L Li, G Zanoni, X Han… - Chemistry–A European …, 2022 - Wiley Online Library
The direct gem‐difluoroalkenylation of X− H bonds represents the most straightforward
approach to access heteroatomic gem‐difluoroalkenes that, as the isostere of the carbonyl …

Catalysts' evolution in the asymmetric conjugate addition of nitroalkanes to electron-poor alkenes

R Ballini, A Palmieri, M Petrini - Organic Chemistry Frontiers, 2022 - pubs.rsc.org
The conjugate addition of nitroalkanes to electron-poor alkenes is a widely used process
which only in the late nineties of the last century has efficiently evolved in its asymmetric …