Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.

Bioorg Med Chem Lett

Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections, de l'Immunité et du Cancer, IICiMed UPRES EA 1155, Faculté de Pharmacie, Nantes, France.

Published: September 2010

AI Article Synopsis

  • Researchers synthesized N-aryl-3-(indol-3-yl)propanamides and tested their immunosuppressive effects.
  • The compound 3-[1-(4-chlorobenzyl)-1H-indol-3-yl]-N-(4-nitrophenyl)propanamide 15 showed strong effectiveness in inhibiting the proliferation of murine splenocytes in lab tests.
  • Additionally, it exhibited significant immunosuppressive activity in a live mouse model, demonstrating its potential for further development.

Article Abstract

N-aryl-3-(indol-3-yl)propanamides were synthesized and their immunosuppressive activities were evaluated. This study highlighted the promising potency of 3-[1-(4-chlorobenzyl)-1H-indol-3-yl]-N-(4-nitrophenyl)propanamide 15 which exhibited a significant inhibitory activity on murine splenocytes proliferation assay in vitro and on mice delayed-type hypersensitivity (DTH) assay in vivo.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2010.07.001DOI Listing

Publication Analysis

Top Keywords

immunosuppressive activities
8
synthesis n-aryl-3-indol-3-ylpropanamides
4
n-aryl-3-indol-3-ylpropanamides immunosuppressive
4
activities n-aryl-3-indol-3-ylpropanamides
4
n-aryl-3-indol-3-ylpropanamides synthesized
4
synthesized immunosuppressive
4
activities evaluated
4
evaluated study
4
study highlighted
4
highlighted promising
4

Similar Publications

LRP4 mutations promote tumour progression and resistance to anti-PD-1 therapy in recurrent hepatocellular carcinoma.

Hepatology

December 2024

Department of Liver Surgery and Transplantation, Zhongshan Hospital, Fudan University, Shanghai 200032, China.

Background And Aims: Hepatocellular carcinoma (HCC) recurrence is a major factor limiting long-time survival and the cause of most deaths in patients with HCC. However, molecular characterisation and potential therapeutic targets of recurrent HCC remain mostly unknown.

Approach And Results: We performed whole-exome sequencing (WES) in 63 matched primary and recurrent HCC tumours and combined the data with whole-genome sequencing (WGS) results in 43 paired samples from our previous study.

View Article and Find Full Text PDF

Epilepsy affects at least 1% of the global population of all socioeconomic backgrounds. Data obtained from previous studies suggest the role of mTOR signaling in epileptogenesis. The present study aimed to investigate the hypothesis that mTOR inhibitor sulfamethizole might produce antiepileptic effects in pentylenetetrazole (PTZ)-induced kindling seizures in mice.

View Article and Find Full Text PDF

Background: The cancer cell marker poliovirus receptor-like protein 4 (PVRL4) has been shown to be highly expressed in many cancers, including lung cancer. Myeloid-derived suppressor cells (MDSCs) are a population of immature myeloid cells with immunosuppressive roles that can attenuate the anticancer response. Here, the precise functions and the relationship between PVRL4 and MDSCs in lung adenocarcinoma (LUAD) progression were investigated.

View Article and Find Full Text PDF

What is new in the pathogenesis and treatment of IgA glomerulonephritis.

World J Nephrol

December 2024

Division of Nephrology, San Giovanni di Dio Hospital, Florence 50143, Toscana, Italy.

Recently, new findings have been clarified concerning both pathogenesis and treatment of IgA nephritis. The four hits theory has been confirmed but several genetic wide association studies have allowed finding several genes connected with the pathogenesis of the disease. All these new genes apply to each of the four hits.

View Article and Find Full Text PDF

Rituximab is an anti-CD20 monoclonal antibody medication used in treating various cancers like non-Hodgkin lymphomas as well as immunologic conditions like granulomatosis with polyangiitis. It disrupts and decreases the number of B-cells, which causes an immunosuppressive state. This can promote the growth of numerous rare and opportunistic pathogens, one of which is .

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!