Design, synthesis, and antitumor activity of desmosdumotin C analogues.

J Asian Nat Prod Res

b Department of Pharmacy , Beijing 100101 , China.

Published: July 2019

Desmosdumotin C (Des C), a natural product isolated from the roots of , has shown good antitumor activity. A three dimensional quantitative structure-activity relationship (QSAR) study using the comparative molecular field analysis (CoMFA) method was performed on 32 Des C analogues. Based on the QSAR, 18 new Des C analogues were designed and synthesized. An efficient three-step synthetic strategy toward Des C and its analogues was developed from commercial available 2, 4, 6-trihydroxyacetophenone. All synthesized compounds were evaluated against a panel of human cancer cell lines and showed ED values ranging from 1.1 to 25.1 µΜ.

Download full-text PDF

Source
http://dx.doi.org/10.1080/10286020.2018.1473383DOI Listing

Publication Analysis

Top Keywords

des analogues
12
antitumor activity
8
design synthesis
4
synthesis antitumor
4
activity desmosdumotin
4
analogues
4
desmosdumotin analogues
4
analogues desmosdumotin
4
des
4
desmosdumotin des
4

Similar Publications

Diabetes represents a significant global health challenge associated with substantial healthcare costs and therapeutic complexities. Current diabetes therapies often entail adverse effects, necessitating the exploration of novel agents. Glucokinase (GK), a key enzyme in glucose homeostasis, primarily regulates blood glucose levels in hepatocytes and pancreatic cells.

View Article and Find Full Text PDF

Water-assisted electrocatalytic oxidation of alcohols into valuable chemicals is a promising strategy to circumvent the sluggish kinetics of water oxidation, while also reducing cell voltage and improving energy efficiency. Recently, transition metal (TM)-based catalysts have been investigated for anodic alcohol oxidation, but success has been limited due to competition from the oxygen evolution reaction (OER) within the working regime. In this study, NiCo-based Prussian blue analog (PBA) was electrochemically activated at the anodic potential to produce a Co-Ni(O)OH active catalyst with a nanosheet-like architecture.

View Article and Find Full Text PDF

Background: Conflicting results have been reported on the impact of tenofovir versus entecavir on liver-related outcomes.

Aims: To explore trends in clinical outcomes in chronic hepatitis B virus (HBV)-infected patients and compare the impact of tenofovir versus entecavir on the risk of hepatocellular carcinoma (HCC), liver transplantation (LT) and mortality.

Methods: We used the French National Health Insurance Databases (SNDS) to identify HBV-infected patients.

View Article and Find Full Text PDF

Introduction: Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by an overactive immune response, particularly involving excessive production of type I interferons. This overproduction is driven by the phosphorylation of IRF7, a crucial factor in interferon gene activation. Current treatments for SLE are often not very effective and can have serious side effects.

View Article and Find Full Text PDF

The walnut tree as a source of progesterone for reproductive control in goats.

Animal

December 2024

Physiologie de la Reproduction et des Comportements, CNRS, INRAE, Université de Tours, 37380 Nouzilly, France.

Intravaginal sponges impregnated with the progesterone (P4) analogue fluorogestone acetate (FGA) induce synchronous oestrous behaviour and normal ovulatory cycle in goats. To explore alternatives using natural P4 from plants, we developed a method of ethanolic extraction and a specific enzyme immunoassay (EIA) to measure P4 in the different parts of the walnut tree Juglans regia. We found a very high concentration of P4, specifically in the leaves of the three most common French varieties (∼100 mg/kg of DM) but not in flowers, fruits, septa, husk, oil or cake.

View Article and Find Full Text PDF

Want 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!