Synthesis and antitumor activity of camptothecin- 4β-triazolopodophyllotoxin conjugates.

Nat Prod Res

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China.

Published: August 2020

Two new compounds ( and ) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound showed highly potent against HL-60 cell line tested, with IC value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development. [Formula: see text].

Download full-text PDF

Source
http://dx.doi.org/10.1080/14786419.2018.1538223DOI Listing

Publication Analysis

Top Keywords

synthesis antitumor
4
antitumor activity
4
activity camptothecin-
4
camptothecin- 4β-triazolopodophyllotoxin
4
4β-triazolopodophyllotoxin conjugates
4
conjugates compounds
4
compounds camptothecin
4
camptothecin cpt
4
cpt analog
4
analog conjugated
4

Similar Publications

CD73, an ectoenzyme responsible for adenosine production, is often elevated in immuno-suppressive tumor environments. Inhibition of CD73 activity holds great promise as a therapeutic strategy for CD73-expressing cancers. In this study, we have developed a therapeutic anti-human CD73 antibody cocktail, HB0045.

View Article and Find Full Text PDF

Inflammasomes are defense complexes that utilize cytokines and immunogenic cell death (ICD) to stimulate the immune system against pathogens. Inspired by their dual action, we present cytokine-armed pyroptosis as a strategy for boosting immune response against diverse types of tumors. To induce pyroptosis, we utilize designed tightly regulated gasdermin D variants comprising different pore-forming capabilities and diverse modes of activation, representing a toolbox of ICD inducers.

View Article and Find Full Text PDF

Secondary lymphedema is a common sequel of oncologic surgery and presents a global health burden still lacking pharmacological treatment. The infiltration of the lymphedematous extremities with CD4T cells influences lymphedema onset and emerges as a promising therapy target. Here, we show that the modulation of CD4FOXP3CD25regulatory T (T) cells upon anti-CTLA4 treatment protects against lymphedema development in patients with melanoma and in a mouse lymphedema model.

View Article and Find Full Text PDF

Metaplastic breast cancer (MpBC) is a highly chemoresistant subtype of breast cancer with no standardized therapy options. A clinical study in anthracycline-refractory MpBC patients suggested that nitric oxide synthase (NOS) inhibitor NG-monomethyl-l-arginine (L-NMMA) may augment anti-tumor efficacy of taxane. We report that NOS blockade potentiated response of human MpBC cell lines and tumors to phosphoinositide 3-kinase (PI3K) inhibitor alpelisib and taxane.

View Article and Find Full Text PDF

Background: TFE3-translocation renal cell carcinoma (TFE3-tRCC), a distinct subtype of kidney cancer characterized by Xp11.2 translocations, involving TFE3 fusion with various partner genes, lacks effective treatments and prognostic biomarkers for advanced stages. This study aimed to unravel the pathogenic mechanisms and uncover novel therapeutic targets.

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!