In previous studies, we have identified a family of benzo[b]furan and benzo[b]thiophene derivatives linked to amino sugars (1-6) that are cytotoxic to a range of cancer cell lines. We describe here an exploration of the effect of structural modification of the amino group on one of the carbohydrate residues (4-amino-2,3,4,6-tetradeoxy-α-l-threo-hexopyranoside) on in vitro cytotoxicity. It has been found that maintaining at least one basic functional group around the C-4 position in the carbohydrate moiety is crucial for cytotoxicity. Furthermore, it appears that modifications around the C-4 position are limited by suitable hydrophilic/hydrophobic and/or ionic interactions, as well as steric constraints.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2011.02.051 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Metabolic profiles of meconium in preeclamptic and normotensive pregnancies.
Metabolomics
January 2025
Center for Child, Adolescent and Maternal Health Research, Faculty of Medicine and Health Technology, Tampere University, Tampere, Finland.
Introduction: Preeclampsia (PE) is a common vascular pregnancy disorder affecting maternal and fetal metabolism with severe immediate and long-term consequences in mothers and infants. During pregnancy, metabolites in the maternal circulation pass through the placenta to the fetus. Meconium, a first stool of the neonate, offers a view to maternal and fetoplacental unit metabolism and could add to knowledge on the effects of PE on the fetus and newborn.
View Article and Find Full Text PDFBranched-chain amino acids and specific phosphatidylinositols are plasma metabolite pairs associated with menstrual pain severity.
Sci Rep
January 2025
Center for Cancer Immunotherapy and Immunobiology, Kyoto University Graduate School of Medicine, Kyoto, Japan.
Menstrual pain affects women's quality of life and productivity, yet objective molecular markers for its severity have not been established owing to the variability in blood levels and chemical properties of potential markers such as plasma steroid hormones, lipid mediators, and hydrophilic metabolites. To address this, we conducted a metabolomics study using five analytical methods to identify biomarkers that differentiate menstrual pain severity. This study included 20 women, divided into mild (N = 12) and severe (N = 8) pain groups based on their numerical pain rating scale.
View Article and Find Full Text PDFDiscarded floral foam as a source for green preparation of sustainable adsorbent for quick and efficient removal of phenoxyacetic acid herbicides from waters.
J Hazard Mater
January 2025
College of the Environment and Ecology, Xiamen University, Xiamen 361005, China; Fujian Provincial Key Laboratory for Coastal Ecology and Environmental Studies, Xiamen University, Xiamen 361005, China. Electronic address:
Due to the high toxicity and increasing consumption, efficient removal of phenoxyacetic acid herbicides (PAAHs) from water is imperative. In current study, a new adsorbent was prepared by modifying porous carbon derived from disused floral foam with chitosan (CS) (ACFC). Density functional theory (DFT) calculation uncovered that the amino and hydroxyl groups in the introduced CS played a critical role in the efficient adsorption of ACFC towards PAAHs.
View Article and Find Full Text PDFCharacterization of a cell-adapted completely attenuated genotype GIIa porcine epidemic diarrhea virus strain.
Virology
January 2025
State Key Laboratory for Animal Disease Control and Prevention, College of Veterinary Medicine, Lanzhou University, Lanzhou Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Lanzhou, 730046, China; Gansu Province Research Center for Basic Disciplines of Pathogen Biology, Lanzhou, 730046, China. Electronic address:
Porcine epidemic diarrhea virus (PEDV) has caused significant harm to the global pig industry since its discovery. In this study, a highly pathogenic strain of GIIa PEDV CH/HBXT/2018, isolated previously, was continuously passaged in Vero cells up to passage (P)240, resulting in a completely attenuated virus. The proliferation characteristics of different passages of the strain in Vero cells, pathogenicity in newborn piglets, and mutations in S gene sequence indicated that as the passage number increased, the replication efficiency of PEDV in Vero cells gradually improved, with a more pronounced cytopathic effect.
View Article and Find Full Text PDFEvaluation of SB-83, a 2-amino-thiophene derivative, against Leishmania species that cause visceral leishmaniasis.
Int Immunopharmacol
January 2025
Infectious Diseases Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brazil. Electronic address:
Visceral leishmaniasis is a systemic disease that affects various internal organs and represents the most severe and fatal form of leishmaniasis. Conventional treatment presents significant challenges, such as prolonged management in hospital settings, high toxicity, and an increasing growing number of cases of resistance. In previous studies, our research group demonstrated the effective and selective activity of the 2-amino-thiophene derivative SB-83 in preclinical models of cutaneous leishmaniasis.
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!