Results 121 to 130 of about 11,521 (228)

Unravelling the Antifibrinolytic Mechanism of Action of the 1,2,3-Triazole Derivatives

International Journal of Molecular Sciences
A new family of antifibrinolytic drugs has been recently discovered, combining a triazole moiety, an oxadiazolone, and a terminal amine. Two of the molecules of this family have shown activity that is greater than or similar to that of tranexamic acid (TXA), the current antifibrinolytic gold standard, which has been associated with several side effects
Yvette Rabadà, Oriol Bosch-Sanz, Xevi Biarnés, Javier Pedreño, Luis Caveda, David Sánchez-García, Jordi Martorell, Mercedes Balcells   +7 more
openaire   +2 more sources

Harnessing Nature: Computational and Experimental Insights Into Ipomoea obscura Metabolites for Bladder Cancer Therapy

Chemistry &Biodiversity, EarlyView.
ABSTRACT Ipomoea obscura (L.), a medicinal plant from the Convolvulaceae family, has been traditionally used to treat various ailments. This study evaluated the in vitro cytotoxicity of its ethanolic leaf extract against human bladder cancer T24 cells and investigated its phytochemical constituents through computational methods.
Saravana Prabha Poochi, Rajamanikandan Sundarraj, Manikandan Vani Raju, Meenakshi Kaniyur Chandrasekaran, Rathi Muthaiyan Ahalliya, Chella Perumal Palanisamy, Gopalakrishnan Velliyur Kanniappan, Benod Kumar Kondapavuluri, Muthu Thiruvengadam   +8 more
wiley   +1 more source

Design, Synthesis, and Molecular Docking of Triazole‐Coumarin Hybrids as Potent Breast Cancer Inhibitors Targeting Cell Cycle and Apoptosis

Chemistry &Biodiversity, EarlyView.
Triazole‐coumarin hybrids were synthesized as breast cancer inhibitors. Derivative 5f induced S‐phase arrest and apoptosis in cancer cells, with minimal toxicity to healthy cells, showing promise for anticancer drug development. ABSTRACT Breast cancer continues to pose a significant global health burden, highlighting the urgent need for novel ...
Murat Keser, Emre Menteşe, Suleyman Ilhan, Mustafa Emirik, Harika Atmaca   +4 more
wiley   +1 more source

1, 2, 3 - Triazoles as key frameworks in drug discovery & metal catalysis [PDF]

, 2017
356 p.La tesis se enmarca dentro de la química de los 1H-1,2,3-triazoles y sus sales de N-alquil-triazolio. El trabajo realizado contempla los siguientes objetivos:1.- Sintetizar y estudiar los 1H-1,2,3-triazoles como plantillas moleculares de fármacos ...
Irastorza Epelde, Aitziber
core  

[1-(2,5-Dichloroanilino)-5-methyl-1H-1,2,3-triazol-4-yl]methanol [PDF]

, 2016
In the title compound, C10H10Cl2N4O, the hy­droxy group and benzene ring are disposed to opposite sides of the central 1,2,3-triazolyl ring. The dihedral angle between the five- and six-membered rings is 87.51 (12)°, and the C-O bond of the hy­droxy ...
Almeida, Maria C. B. de, Cunha, Anna C., Ferreira, Vitor F., Jordão, Alessandro K., Souza, Maria C. B. V. de, Tiekink, Edward R. T. *, Wardell, James L.   +6 more
core   +2 more sources

Recent Advances in Isatin–Thiazole Hybrids: Synthesis, Structural Design, and Biological Application

Chemistry &Biodiversity, EarlyView.
ABSTRACT Isatin–thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin–thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years ...
Isadora M. G. Andrade, Edson de O. Lima Filho, Caio F. Valadão, Luana da S. M. Forezi, Fernando de C. da Silva   +4 more
wiley   +1 more source

Poly(ethylene Glycol)‐Based Peptidomimetics (Pegtides) of Antimicrobial Peptides

ChemBioChem, EarlyView.
Polyethylene glycol (PEG) is commonly used to improve the pharmacokinetics and pharmacodynamics of therapeutic candidates by conjugation. Here PEG is exploited for peptidomimetic conversion of antimicrobial peptides (AMPs), as candidate antibacterial agents, by replacing their polyamide backbone. The pegtides obtained thereby can be readily synthesized
Conor Shine, John R. F. B. Connolly, Robert D. Murphy, Hazel Lafferty, Abdalmalek Alfnikh, Ned P. Buijs, Hawraa Shahrour, Nathaniel I. Martin, Eoghan O'Neill, George Amarandei, Jimmy Muldoon, Marc Maresca, Deirdre Fitzgerald‐Hughes, Marc Devocelle   +13 more
wiley   +1 more source

Biocompatible Chemistry: A Plug‐and‐Play Toolbox for Chemical Biology Research

ChemBioChem, EarlyView.
The “plug‐and‐play” nature of biocompatible chemistry makes it a powerful toolbox for investigating complicated biological systems and producing drug leads for clinical usages. This review summarizes the commonly used biocompatible reactions and the recent advances of their representative applications in chemical biology research, thus highlighting the
Adam R. Lovato, Zeng Lin, Qingfei Zheng
wiley   +1 more source

Synthèse, dérivation et évaluation de pharmacophores hybrides Alcynyl-TriAzolyCarbinols N-glycosylés [PDF]

, 2014
La fonction alcényl-alcynylcarbinol (AAC) est un pharmacophore clé rencontré dans des produits naturels extraits d'éponges marines, les pétrosiacétylènes, aux propriétés biologiques multiples, en particulier une cytotoxicité remarquable sur les cellules ...
Oukessou, Mohamed
core  

Insulin-like Growth Factor 1 Analogs Clicked in the C Domain : Chemical Synthesis and Biological Activities [PDF]

, 2017
Human insulin-like growth factor 1 (IGF-1) is a 70 amino acid protein hormone, with key impact on growth, development, and lifespan. The physiological and clinical importance of IGF-1 prompted challenging chemical and biological trials toward the ...
Andrzej M. Brzozowski, Bayne M. L., Du Y. C., Irena Selicharová, Jan Pícha, Jiří Jiráček, Kateřina Macháčková, Lenka Žáková, Martina Chrudinová, Michaela Collinsová, Miloš Buděšínský, Václav Vaněk   +11 more
core   +2 more sources