A possible inhibitor of proteases, which contains an indole core and an aromatic polar acetylene, was designed and synthesized. This indole derivative has a molecular architecture kindred to biologically relevant species and was obtained through five synthetic steps with an overall yield of 37% from the 2,2'-(phenylazanediyl)di(ethan-1-ol). The indole derivative was evaluated through docking assays using the main protease (SARS-CoV-2-M) as a molecular target, which plays a key role in the replication process of this virus. Additionally, the indole derivative was evaluated as an inhibitor of the enzyme kallikrein 5 (KLK5), which is a serine protease that can be considered as an anticancer drug target.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8270299 | PMC |
| http://dx.doi.org/10.3390/molecules26133817 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Unfolding the Potential of Pyrrole- and Indole-Based Allylidene Hydrazine Carboximidamides as Antimicrobial Agents.
ACS Infect Dis
January 2025
Pharmaceutical Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Pilani, Vidya Vihar 333031, (RJ) India.
Antimicrobial drug resistance is a significant global health challenge, causing hundreds of thousands of deaths annually and severely impacting healthcare systems worldwide. Several reported antimicrobial compounds have a guanidine motif, as the positive charge on guanidine promotes cell lysis. Therefore, pyrrole- and indole-based allylidene hydrazine carboximidamide derivatives with guanidine motifs are proposed as antimicrobial agents that mimic cationic antimicrobial peptides (CAMPs).
View Article and Find Full Text PDFEngineered Perfluorochemical Cancer-Derived Exosomes Loaded with Indocyanine Green and Camptothecin Provide Targeted Photochemotherapy for Effective Cancer Treatment.
Int J Nanomedicine
January 2025
Department of Biomedical Sciences and Engineering, National Central University, Taoyuan City, Taiwan, Republic of China.
Background: Cancer treatments are still limited by various challenges, such as off-target drug delivery, posttreatment inflammation, and the hypoxic conditions in the tumor microenvironment; thus, the development of effective therapeutics remains highly desirable. Exosomes are extracellular vesicles with a size of 30-200 nm that have been widely applied as drug carriers over the last decade. In this study, melanoma-derived exosomes were used to develop a perfluorocarbon (PFC) drug nanocarriers loaded with indocyanine green (ICG) and camptothecin (CPT) (ICFESs) for targeted cancer photochemotherapy.
View Article and Find Full Text PDFNeuroprotective Indole Alkaloids from the Soil-Derived Fungus sp. XZ8.
J Nat Prod
January 2025
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry and Pharmacy, Northwest A&F University, Yangling, Shaanxi 712100, People's Republic of China.
A chemical investigation of the soil-derived fungus sp. XZ8 led to the isolation of five new indole alkaloids, trichindoles A-E (-), with diverse architectures, along with seven known analogues (-). Their structures were elucidated by extensive spectroscopic data analysis, and their absolute configurations were determined by single-crystal X-ray diffraction and modified Mosher's method.
View Article and Find Full Text PDFAttraction of Bactrocera cucurbitae (Coquillett) to selected gut microbiota supernatants: implications for pest control.
Pest Manag Sci
January 2025
State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing, China.
Background: Bactrocera cucurbitae (Coquillett) is a distructive quarantine insect pest that causes significant economic losses on cucurbit crops. To explore a green control approach, we investigated the behavioral responses of B. cucurbitae larvae and adults to bacterial suspensions, sediments, and supernatants derived from eight gut microbial strains across four distinct genera.
View Article and Find Full Text PDFIntegrated Transcriptome and Metabolome Analysis Reveals the Resistance Mechanisms of Against .
Int J Mol Sci
January 2025
Key Laboratory of Biology and Genetics Improvement of Oil Crops, Oil Crops Research Institute of Chinese Academy of Agricultural Sciences, Ministry of Agriculture and Rural Affairs, Wuhan 430062, China.
Rapeseed ( L.) is an important crop for healthy edible oil and stockfeed worldwide. However, its growth and yield are severely hampered by black rot, a destructive disease caused by pv.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!