Rational discovery of novel phenylindole-bisamide derivatives as potent P-glycoprotein inhibitors for cancer multidrug resistance [0.03%]
Zhikun Yang,Jiajia Han,Yanhong Yang et al.
Zhikun Yang et al.
Overcoming multidrug resistance (MDR) remains a major challenge in cancer chemotherapy, largely mediated by the efflux pump P-glycoprotein (P-gp). To address this, we designed and synthesized a series of novel phenylindole-bisamide derivati...
Adamantane-based inhibitors of the influenza A M2 proton channel: structure-based design, biological evaluation, and synthetic approaches [0.03%]
Marianna Stampolaki,Maria-Eleni Kouridaki,Kyriakos Georgiou et al.
Marianna Stampolaki et al.
The influenza A matrix 2 (AM2) protein, a prototype of viroporins, conducts protons along a chain of water molecules and ionizable side chains, including histidine-37. Solid-state NMR (ssNMR) and high-resolution X-ray crystal structures hav...
Exploration of a benzothiophene scaffold for use as adjuvants with β-lactam antibiotics against methicillin-resistant Staphylococcus aureus [0.03%]
Monica A Stefaniak,Vijay S Gondil,Emily P Gillis et al.
Monica A Stefaniak et al.
Rising antibiotic resistance coupled with diminishing investment in antibiotic development has led to limited treatment options for multi drug-resistant bacterial infections. Penicillin binding protein 2a (PBP2a) is a key determinant of res...
From bolinaquinone, a marine hydroxyquinone sesquiterpene, to naphthoquinones with clathrin inhibitory effects [0.03%]
Nicholas S O&#x;Brien,Azadeh Ghods,Jing Xue et al.
Nicholas S O&#x;Brien et al.
Bolinaquinone (BLQ, 1), a hydroxyquinone sesquiterpene, has been reported to inhibit clathrin mediated endocytosis. As there is no reported clathrin IC50 or commercial source of BLQ, we examined the related marine hydroxysesquiterpenes (5-1...
Extending the architecture of bolaamphiphilic disinfectants: an investigation of octenidine and isooctenidine analogs [0.03%]
Danielle E Talbot,Caroline M Casey,Elise L Bezold et al.
Danielle E Talbot et al.
Quaternary ammonium compounds (QACs) have been used in commercial disinfectants since the mid-1900s due to their strong antimicrobial activity and relatively low toxicity to eukaryotic cells. However, antimicrobial resistance to common disi...
The effects of bioisostere substitution on the antimicrobial and physicochemical properties of supramolecular self-associating amphiphiles [0.03%]
Pinky K Naicker,Mariam Yacoub,Lisa J White et al.
Pinky K Naicker et al.
The rise of antimicrobial resistance (AMR) is one of the greatest health threats facing the world today. Supramolecular self-associating amphiphiles (SSAs) have shown potential for development as novel antimicrobial agents. We now move to e...
Design, synthesis and biological evaluation of benzoyl hydrazone derivatives as anticancer agents inducing ROS-associated mitochondrial apoptosis [0.03%]
Rongbin Wei,Xin Wang,Yamin Ding et al.
Rongbin Wei et al.
Cancer, due to its high morbidity and mortality rate, coupled with the dose-restricted toxicity of many chemotherapy drugs, is still a major challenge in the global health field. In order to meet this challenge, we report the design and syn...
New series of pentamidine-based 1,2,3-triazole-diaryl-hydrazones: design, synthesis, and evaluation of their leishmanicidal activity and mechanism of action against Leishmania (L.) amazonensis [0.03%]
Patrícia F Espuri Sepini,Vanessa Silva Gontijo,Laiane Mota Tavares et al.
Patrícia F Espuri Sepini et al.
Leishmaniasis is caused by over twenty Leishmania species worldwide. Current chemotherapy is limited to a few approved drugs, with high toxicity and significant side effects, and compromised efficacy due to parasite resistance. pentamidine ...
Verbenone-based selenophene derivatives as potential anti-cancer agents: synthesis and biological evaluation in 2D and 3D A549 cell models [0.03%]
Jiale Han,Wei Shi,Min Hu et al.
Jiale Han et al.
Natural product inspired scaffolds remain a valuable source of novel anticancer agents. In this study, a series of verbenone-selenophene derivatives (2A-2U) were rationally designed and synthesized. Their antiproliferative activities were e...
Design and biological evaluation of triagonist GLP-1R/GCGR/GIPR peptides as potential therapeutic agents for diabetes and obesity [0.03%]
Iwona Kalinowska,Alicja Gawalska,Paulina Kasprzycka et al.
Iwona Kalinowska et al.
Obesity and type 2 diabetes have reached pandemic proportions, largely driven by sedentary lifestyles and unhealthy dietary habits. According to the World Obesity Atlas 2024, by 2035 more than 4 billion adults and children are expected to b...