Recent update on development of small-molecule STAT3 inhibitors for cancer therapy: from phosphorylation inhibition to protein degradation

J Dong, XD Cheng, WD Zhang… - Journal of Medicinal …, 2021 - ACS Publications
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that
regulates various biological processes, including proliferation, metastasis, angiogenesis …

Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?

Q Huang, Y Zhong, H Dong, Q Zheng, S Shi… - European Journal of …, 2020 - Elsevier
As a transcription factor, STAT3 protein transduces extracellular signals to the nucleus and
then activates transcription of target genes. STAT3 has been well validated as an attractive …

Reversible spatiotemporal control of induced protein degradation by bistable PhotoPROTACs

P Pfaff, KTG Samarasinghe, CM Crews… - ACS Central …, 2019 - ACS Publications
Off-tissue effects are persistent issues of modern inhibition-based therapies. By merging the
strategies of photopharmacology and small-molecule degraders, we introduce a novel …

Visible-light-controlled histone deacetylase inhibitors for targeted cancer therapy

L Josa-Culleré, A Llebaria - Journal of medicinal chemistry, 2023 - ACS Publications
The lack of selectivity of anticancer drugs limits current chemotherapy. Light-activatable
drugs, whose activity can be precisely controlled with external light, could provide a more …

[HTML][HTML] Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo

P Yue, Y Zhu, C Brotherton-Pleiss, W Fu, N Verma… - Cancer letters, 2022 - Elsevier
Signal transducer and activator of transcription (Stat) 3 is a valid anticancer therapeutic
target. We have discovered a highly potent chemotype that amplifies the Stat3-inhibitory …

Discovery of novel azetidine amides as potent small-molecule STAT3 inhibitors

C Brotherton-Pleiss, P Yue, Y Zhu… - Journal of Medicinal …, 2020 - ACS Publications
We optimized our previously reported proline-based STAT3 inhibitors into an exciting new
series of (R)-azetidine-2-carboxamide analogues that have sub-micromolar potencies. 5a …

Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3-and 4-membered N-heterocyclic scaffolds

D Łowicki, P Przybylski - European Journal of Medicinal Chemistry, 2022 - Elsevier
Cascade reactions are often 'employed'by nature to construct structurally diverse nitrogen-
containing heterocycles in a highly stereoselective fashion, ie, secondary metabolites …

Boronic acid: a novel pharmacophore targeting src homology 2 (SH2) domain of STAT3

L Deng, J Mo, Y Zhang, K Peng, H Li… - Journal of Medicinal …, 2022 - ACS Publications
SH2 domains have been recognized as promising targets for various human diseases.
However, targeting SH2 domains with phosphopeptides or small-molecule inhibitors derived …

Synthesis, characterization and behavior in water/DMSO solution of Ru (II) arene complexes with bioactive carboxylates

L Biancalana, G Pampaloni, S Zacchini… - Journal of Organometallic …, 2018 - Elsevier
The reactions of [RuCl (μ-Cl)(η 6-p-cymene)] 2 with sodium carboxylates, in methanol or
acetonitrile solution, afforded the complexes [RuCl (κ 2 O-RCO 2)(η 6-p-cymene)](RCO 2 …

Structural optimization of Imidazo [1, 2-a] pyridine derivatives for the treatment of gastric cancer via STAT3 signaling pathway

H Li, S Ouyang, Y Zhang, K Peng, W Fang, Z Liu… - European Journal of …, 2022 - Elsevier
STAT3 is a promising therapeutic target for the treatment of gastric cancer, which is one of
the most common solid tumors worldwide. In the previous works, we discovered a series of …