Results 241 to 250 of about 98,614 (298)

Pegargiminase Suppresses the Fanconi Anemia Pathway and Promotes Melphalan‐Induced DNA Double‐Strand Breaks in Uveal Melanoma

Pigment Cell &Melanoma Research, Volume 39, Issue 4, July 2026.
ADI‐PEG20 enhances melphalan‐induced DNA DSBs in UM cells. We describe potentiation of DNA DSBs in UM cell lines upon treatment with ADI‐PEG20 and melphalan (92.1 cells with STRIDE by intoDNA). ADI‐PEG20 suppresses multiple members of the FA pathway—a known resistance mechanism for melphalan—providing a rationale for exploring this drug combination in ...
Iuliia Pavlyk, George Field, Matthew Young, Josephine Carpentier, Emilia A. Szlosarek, Michaela R. O'Keeffe‐Brown, Timothy Crook, Nelofer Syed, John S. Bomalaski, Pui Ying Chan, Peter W. Szlosarek   +10 more
wiley   +1 more source

Structure‐Based Design, Synthesis, and Evaluation of Novel Ponatinib Derivatives With a Significantly Altered Selectivity Profile

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
We developed new derivatives of the cancer drug ponatinib, significantly reducing and altering its spectrum of target kinases. Compound 5 retained the efficacy in inhibiting the colony formation of MDA‐MB‐231 cells and acted primarily on B‐Raf and Flt‐1 as its main targets in a kinase panel.
Tobias Betzholz, Ting Liu, Andreas Krämer, Verena Dederer, Stefan Knapp, Sebastian Mathea, Christian Ducho, Matthias Engel   +7 more
wiley   +1 more source

The E3 ubiquitin ligase, RNF219, suppresses CNOT6L expression to exhibit antiproliferative activity. [PDF]

FEBS Open Bio
Soeda S, Montrose M, Takahashi A, Ishida R, Burriel S, Ohmine N, Natsume T, Adachi S, Kim M, Yamamoto T.   +9 more
europepmc   +1 more source

Design and Synthesis of Pyrimidino[4,5‐d]Pyrimidine‐Based Compounds as Potent B‐RAF V600E Inhibitors

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
Novel pyrimido[4,5‐d]pyrimidine‐based inhibitors selectively target B‐RAF V600E with nanomolar affinity and adopt distinct type‐II binding modes. Complementary cellular profiling reveals highly active analogs, underscoring the versatility of this chemotype and establishing it as a promising scaffold for the development of next‐generation kinase ...
Eleftheria A. Georgiou, Kalliopi Christopoulou, Amalia D. Kalampaliki, Aikaterini F. Giannopoulou, Eleftheria Chatziorfanou, Vivi Bafiti, Andreas Krämer, Athanasios Papakyriakou, Dimitrios J. Stravopodis, Stefan Knapp, Ioannis K. Kostakis   +10 more
wiley   +1 more source

Agar Composition Modulates Production of Trichoderma Peptaibols, Affecting Antibacterial and Antiproliferative Activity. [PDF]

Curr Microbiol
Macášek P, Kapustová A, Viktorová J, Víglaš J, Olejníková P, Grey L, Laubertová L, Gbelcová H.   +7 more
europepmc   +1 more source

Probing 3‐Amino‐2H‐Azaindazoles as Allosteric Inhibitors of the Protein Tyrosine Phosphatase SHP2

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
A palladium‐catalyzed domino reaction facilitated the discovery and rapid synthesis of selective, potent 3‐amino‐2H‐azaindazole derivatives serving as allosteric inhibitors of SHP2. Structural analysis via co‐crystallography confirmed binding at the allosteric site, thereby stabilizing the autoinhibited SHP2 conformation, qualifying this scaffold as a ...
Machoud Amoussa, Nina‐Louisa Efrém, Feng Li, Ziqiong Guo, Yvette Roske, Katrin Jana Frank, Szymon Pach, Clemens Alexander Wolf, Feng Bo, Marina Lesina, Mika Kintzel, Rana Alsalim, Victoria Zeitz, Noémi Csorba, Silke Radetzki, György M. Keserű, Oliver Daumke, Hana Algül, Gerhard Wolber, Jia Li, Marc Nazaré   +20 more
wiley   +1 more source

Total Synthesis and Antimalarial Studies of Caelestines A–C

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
Total synthesis of caelestines A–C (alkaloids from the Australian ascidian, Aplidium caelestis) was accomplished, constituting the first synthesis of caelestines B and C. Caelestines A–C, with five other novel quinolones, were assessed against Plasmodium falciparum 3D7 and Dd2. Caelestine B was found to be a selective antimalarial alkaloid. Caelestines
Henry S. T. Smith, Aaron M. Lock, Vicky M. Avery, Rohan A. Davis   +3 more
wiley   +1 more source

Increased Antiproliferative Activity of Antiestrogens and Neratinib Treatment by Calcitriol in HER2-Positive Breast Cancer Cells. [PDF]

Int J Mol Sci
Milo-Rocha E, Díaz L, García-Quiroz J, Prado-Garcia H, García-Becerra R.   +4 more
europepmc   +1 more source

Stereochemical Modulation of Palladacyclopentadienyl Complexes Bearing Diphosphine Ligands: A Key to Enhanced DNA Interaction and Anticancer Activity

European Journal of Inorganic Chemistry, Volume 29, Issue 16, 4 June 2026.
A modular library of structurally robust palladacyclopentadienyl Pd(II) complexes bearing achiral and chiral diphosphines was developed, revealing a strong influence of diphosphine design and ligand chirality on cytotoxicity and selectivity against ovarian cancer cells, including platinum‐resistant models.
Stefania Mautone, Martina Scianna, Isabella Caligiuri, Laura Orian, Pablo Nogara, Nicola Demitri, Flavio Rizzolio, Thomas Scattolin   +7 more
wiley   +1 more source

Monothiooxalamide-Benzothiazole Hybrids: Predictive Docking on HDAC6, Synthesis, Molecular Structure, and Antiproliferative Activity on Breast Cancer Cells. [PDF]

Int J Mol Sci
Macías-Hernández CE, Balbuena-Rebolledo I, García-Báez EV, Cabrera-Pérez LC, Godínez-Victoria M, Rosales-Hernández MC, Padilla-Martínez II.   +6 more
europepmc   +1 more source