Results 41 to 50 of about 1,668,623 (259)

Novel indole-based synthetic molecules in cancer treatment: Synthetic strategies and structure-activity relationship

Medicine in Drug Discovery
Indole is one of the naturally occurring nitrogen-containing bicyclic heterocyclic ring systems where benzene and pyrrole rings are fused. It has been demonstrated to exhibit versatile biological activities.
Biplab Debnath, Bikram Nandi, Samiran Paul, Swarup Manna, Arindam Maity, Krishnalekha Bandyopadhyay, Shambo Panda, Shah Alam Khan, Rajarshi Nath, Md Jawaid Akhtar   +9 more
doaj   +1 more source

Indole derivatives as multifunctional drugs: Synthesis and evaluation of antioxidant, photoprotective and antiproliferative activity of indole hydrazones.

Bioorganic chemistry (Print), 2019
Two series of indole derivatives 4-17, 20-22 were easily prepared and assayed for their radical-scavenging ability. Arylidene-1H-indole-2-carbohydrazones showed different extent antioxidant activity in DPPH, FRAP and ORAC assays.
Monica Demurtas, A. Baldisserotto, I. Lampronti, D. Moi, G. Balboni, S. Pacifico, S. Vertuani, S. Manfredini, V. Onnis   +8 more
semanticscholar   +1 more source

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

Photoredox-Catalyzed Intermolecular Hydroalkylative Dearomatization of Electron-Deficient Indole Derivatives.

Organic Letters, 2020
Dearomatization of indole derivatives offers a straightforward approach to access diverse indolines. To date, the corresponding dearomative transformations involving electron-deficient indoles are limited.
Xuhu Huang, Yuan‐Zheng Cheng, Xiao Zhang, S. You   +3 more
semanticscholar   +1 more source

Establishing an assay to evaluate d‐amino acid oxidase enzyme kinetics and inhibition using WST‐8 redox dye

FEBS Open Bio, EarlyView.
This study investigated a novel WST‐8‐based assay for evaluating d‐Amino acid oxidase (DAO) inhibitors. We confirmed its effectiveness using known inhibitors and found that uremic toxins possess relatively weak inhibitory activity compared to existing drugs.
Kahoko Miyake, Yuki Enoki, Yuka Nakazawa, Kazuaki Taguchi, Kazuaki Matsumoto   +4 more
wiley   +1 more source

The Intestinal Barrier Protective Effect of Indole Aldehyde Derivatives on Acute Toxoplasma gondii Infection

Molecules
Toxoplasmosis, a zoonotic infection caused by Toxoplasma gondii (T. gondii), poses a significant risk to human health and public safety. Despite the availability of clinical treatments, none effectively mitigate the intestinal barrier damage, which is ...
Jieqiong Wang, Weifeng Yan, Xu Cheng, Yonggang Tong, Sihong Wang, Chunmei Jin   +5 more
doaj   +1 more source

Rh(III)‐Catalyzed C‐2 Alkylation of Indoles followed by a Post‐Synthetic Modification via the Ugi Reaction

ChemistryOpen, 2023
Indole derivatives substituted at the C‐2 position have shown important biological activities. Due to these properties, several methods have been described for the preparation of structurally diverse indoles.
Marcelo Augusto Pereira Januário, Demetrius P. deSouza, Prof. Dr. Julio Zukerman‐Schpector, Prof. Dr. Arlene G. Corrêa   +3 more
doaj   +1 more source

Molecular dynamics simulations of positively selected codons in FcγRI reveal novel biochemical binding properties

FEBS Open Bio, EarlyView.
Evolutionary analysis across 32 placental mammals identified positive selection at residues H148 and W149 in the immune receptor FcγR1. Ancestral reconstruction combined with molecular dynamics simulations reveals how these mutations may influence receptor structure and dynamics, providing insight into the evolution of antibody recognition and immune ...
David A. Young, Omar Arias‐Gaguancela, Fiona Gibson, Morgan Grainger, Jodie Score, Amit Nathubhai, Mauricio Cafiero, Lee Richard Machado   +7 more
wiley   +1 more source

New‐Era Polymer Thermoelectrics: Material Innovations, Doping Frontiers, Decoupling Strategies, and Unconventional Applications

Advanced Materials, EarlyView.
The field of polymer thermoelectrics is entering a new era, featuring breakthroughs in addressing the conventional performance disparity between p‐type and n‐type polymers, pioneering doping frontiers, and sophisticated decoupling strategies. This review explores innovations in molecular design and superior stabilities, bridging the gap from ...
Suhao Wang
wiley   +1 more source

Synthesis and biological evaluation of N-substituted indole chalcone derivatives as potent antitubercular agents

Future Journal of Pharmaceutical Sciences
The in vitro antitubercular activity of a new family of N-substituted indole chalcone analogues against Mycobacterium Tuberculosis H37Rv has been synthesized and evaluated.
Shivam Joshi, Neha Kawathekar
doaj   +1 more source