Results 221 to 230 of about 5,874,294 (289)

Artificial Intelligence and Virtual Screening to Identify Small Molecules Inhibiting Transglutaminase 2 for Investigation and Treatment of Breast Cancer

ChemBioChem, Volume 27, Issue 18, 28 September 2026.
Artificial Intelligence (AI)‐guided screening of nearly 10 million molecules hit the bull’s‐eye: G11, a new nonpeptidic inhibitor of transglutaminase 2. A stepwise path from in silico ranking to cell and biochemical assays identified G11 as the top hit. It induced apoptosis in transglutaminase 2 (TG2)‐rich breast cancer cells and inhibited purified TG2,
Carlo M. Bergamini, Niel M. Henriksen, Brianna Ryan, Taylor A. Prince, Anna Terrazzan, Pietro Ancona, Cristina Zuccato, Gianluca Aguiari, Valentina Rosta, Jeffrey W. Keillor, Alessandro Trentini, Nicoletta Bianchi   +11 more
wiley   +1 more source

Capsaicin-Inspired Hydroxamate Hybrids as Selective HDAC6 Inhibitors with Antiproliferative Activity in Hematological Malignancies. [PDF]

ACS Omega
Gimenez Borges L, Alves TNO, Vassiliades SV, Carlos JAEG, Waitman KB, Hilscher S, Schutkowski M, Sippl W, Tavares MT, Toledo MFZJ, Costa-Lotufo LV, Kronenberger T, Machado-Neto JA, Parise-Filho R.   +13 more
europepmc   +1 more source

Design, Synthesis, and Biological Evaluation of Pyrazolyl Thioureas (PTUs) as SIRT1 and SIRT2 Inhibitors

ChemMedChem, Volume 21, Issue 18, 28 September 2026.
Pyrazolyl thioureas were designed and synthesized as sirtuin 1 (SIRT1) and sirtuin 2 (SIRT2) inhibitors. 6a (IC50 (SIRT1) = 5.3 µM; IC50 (SIRT2) = 2.2 µM) and 7f (IC50 (SIRT1) = 12.4 µM; IC50 (SIRT2) = 13.6 µM) showed micromolar inhibition on target enzymes and HepG2‐based assays confirmed a SIRT2‐mediated effect on tubulin acetylation. Docking studies
Matteo Lusardi, Cecilia Astigiano, Deianira Bellitto, Matteo Raineri, Giorgia Guccione, Annalisa Salis, Elena Cichero, Chiara Brullo, Marco Ponassi, Santina Bruzzone, Andrea Spallarossa   +10 more
wiley   +1 more source

In vitro antiproliferative activity on A549 and HT-29 cell lines and fatty acid profiling of Agaricus bresadolanus and A. hortensis. [PDF]

Naturwissenschaften
Alli H, Demir İ, Yeniocak S, Kivrak İ, Sarac N, Kaya E, Ugur A.   +6 more
europepmc   +1 more source

Lysosome‐Targeted Squaramide Anion Transporters

Chemistry – A European Journal, Volume 32, Issue 36, 24 September 2026.
Lysosome‐targeted squaramide anion transporters elicit different biological effects depending on the targeting group employed. ABSTRACT Targeting anion transporters to specific organelles has previously been shown to be an effective strategy to enhance their cytotoxicities against cancerous cell lines.
Elba Feo, Edward York, Anthony Thai, William G. Ryder, Daniel A. McNaughton, Philip A. Gale   +5 more
wiley   +1 more source

Borylcyclopropanes: Synthetic Strategies and Applications

Angewandte Chemie, Volume 138, Issue 37, 7 September 2026.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

Ultrasound-Assisted Synthesis and Biological Profiling of 1,3,5-Triazine Derivatives with Antiproliferative Activity in Triple-Negative Breast Cancer. [PDF]

Curr Issues Mol Biol
Bosak N, Drabczyk AK, Jaśkowska J, Stachowicz-Suhs M, Filip-Psurska B, Boguszewska-Czubara A, Greber KE, Ciura K, Kułaga D.   +8 more
europepmc   +1 more source

(S)‐Pyrrolo[1,2‐a]pyrazine‐3‐carboxamide Analogs as Dual Akt/JNK Modulators With Antiproliferative Effects in MDA‐MB‐468 Cells

ChemMedChem, Volume 21, Issue 17, 14 September 2026.
Among 30 synthesized pyrrolo[1,2‐a]pyrazine analogs, compounds B1 and B3 showed strong and selective cytotoxicity toward TNBC cells, inducing apoptosis through Akt suppression and JNK activation. Triple‐negative breast cancer (TNBC) remains a major clinical challenge due to the absence of effective targeted therapies.
Narges Hosseininasab, Sou Hyun Kim, Ye‐Mi Kwon, Jungjin Park, Chanhyun Jung, Kwanghee Lee, Beom‐Jun Wi, Su‐Jin Yoo, Soonsil Hyun, Young‐Suk Jung, Jae‐Hwan Kwak   +10 more
wiley   +1 more source

Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity. [PDF]

RSC Adv
Saleem BAA, Qurtam AA, Shalabi AR, Al-Zharani M, Abass KS, Bräse S, Alotaibi G, Alkhammash A.   +7 more
europepmc   +1 more source

Piperazine and Morpholine Protoporphyrin IX Derivatives Intensify Biomolecules Oxidation and Phototoxicity in Triple‐Negative Breast Cancer

ChemMedChem, Volume 21, Issue 17, 14 September 2026.
Protoporphyrin IX derivatives bearing piperazine or morpholine substituents exhibit enhanced cellular retention and photodynamic activity in triple‐negative breast cancer cells. Structural modification promotes oxidative stress, alters mitochondrial membrane potential, and increases caspase‐3 activity, providing new structure–activity relationship ...
Maynne Duarte Suriani Franco, Thibault Joseph William Jacques Dit Lapierre, Tarcisio Paiva Mendonça, Luiz Felipe Fernandes Peixoto, Renata Roland Teixeira, Joyce Ferreira Da Costa Guerra, Kelly Aparecida Geraldo Yoneyama Tudini, Daniele Lisboa Ribeiro, Foued Salmen Espindola, Allisson Benetti Justino, Celso de Oliveira Rezende Júnior, Tayana Mazin Tsubone   +11 more
wiley   +1 more source