To design new compounds suitable as starting points for anticancer drug development, we have synthesized a novel series of benzoxazoles with pharmaceutically advantageous piperazine and fluorine moieties attached to them. The newly synthesized benzoxazoles and their corresponding precursors were evaluated for cytotoxicity on human A-549 lung carcinoma cells and non-cancer HepaRG hepatocyes. Some of these new benzoxazoles show potential anticancer activity, while two of the intermediates show lung cancer selective properties at low concentrations where healthy cells are unaffected, indicating a selectivity window for anticancer compounds.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274350 | PMC |
| http://dx.doi.org/10.3390/molecules21101290 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Self-propelling, protein-bound magnetic nanobots for efficient in vitro drug delivery in triple negative breast cancer cells.
Sci Rep
December 2024
Department of Pharmaceutical Chemistry, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India.
The emergence of self-propelling magnetic nanobots represents a significant advancement in the field of drug delivery. These magneto-nanobots offer precise control over drug targeting and possess the capability to navigate deep into tumor tissues, thereby addressing multiple challenges associated with conventional cancer therapies. Here, Fe-GSH-Protein-Dox, a novel self-propelling magnetic nanobot conjugated with a biocompatible protein surface and loaded with doxorubicin for the treatment of triple-negative breast cancer (TNBC), is reported.
View Article and Find Full Text PDFYu-Ping-Feng-San improve the immunosuppression of microenvironment in hepatocellular carcinoma by promoting the maturation of DCs through the JAK2-STAT3 pathway.
Sci Rep
December 2024
Central Laboratory, Suzhou TCM Hospital Affiliated to Nanjing University of Chinese Medicine, Suzhou, 215000, Jiangsu, China.
Yu-Ping-Feng-San (YPF) is a famous classical Chinese medicine formula known for its ability to boost immunity. YPF has been applied to enhance the immune status of tumor patients in clinical practice. However, there is still a lack of research on its immune regulatory effects and mechanisms in the tumor microenvironment.
View Article and Find Full Text PDFPan-cancer association of a mitochondrial function score with genomic alterations and clinical outcome.
Sci Rep
December 2024
Department of Laboratory Medicine, The Affiliated Hospital of Southwest Medical University, Sichuan Province Engineering Technology Research Center of Molecular Diagnosis of Clinical Diseases, Molecular Diagnosis of Clinical Diseases Key Laboratory of Luzhou, Luzhou, Sichuan, China.
Mitochondria are pivotal in cellular energy metabolism and have garnered significant attention for their roles in cancer progression and therapy resistance. Despite this, the functional diversity of mitochondria across various cancer types remains inadequately characterized. This study seeks to fill this knowledge gap by introducing and validating MitoScore-a novel metric designed to quantitatively assess mitochondrial function across a wide array of cancers.
View Article and Find Full Text PDFEffects of water-fertiliser coupling on the photosynthesis and quality of Lycium barbarum based on predicted crop evapotranspiration (ET).
Sci Rep
December 2024
School of Civil and Hydraulic Engineering, Ningxia University, Yinchuan, Ningxia, 750021, China.
Lycium barbarum is an important economic crop in the arid region of Northwest China, and the regulation of irrigation and fertilisation is an important way to improve the quality and yield of Lycium barbarum. To explore the effects of water-fertiliser coupling on photosynthesis, quality and yield of Lycium barbarum under irrigation methods based on predicted crop evapotranspiration (ET), ET was calculated via reference evapotranspiration (ET) predicted on the basis of public weather forecasts, and the irrigation water volume was determined as a proportion of this ET. A field experiment was conducted via a completely randomised experimental design with five irrigation water volumes (W0 (100% ET), W1 (90% ET), W2 (80% ET), W3 (70% ET) and W4 (65% ET)) and three fertiliser application rates (high fertiliser (FH), medium fertiliser (FM) and low fertiliser (FL)).
View Article and Find Full Text PDFHydroxyethylamine based analog targets microtubule assembly: an in silico study for anti-cancerous drug development.
Sci Rep
December 2024
Department of Biotechnology, Mahatma Gandhi Central University, Motihari, 845401, India.
Microtubules are dynamic cytoskeletal structures essential for cell architecture, cellular transport, cell motility, and cell division. Due to their dynamic nature, known as dynamic instability, microtubules can spontaneously switch between phases of growth and shortening. Disruptions in microtubule functions have been implicated in several diseases, including cancer, neurodegenerative disorders such as Alzheimer's and Parkinson's disease, and birth defects.
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!