AMIDES AND S-NITROSOTIOLS DERIVATIVES FROM NON-STOROID ANTI-INFLAMMATORIES: SYNTHESIS IN ENVIRONMENTALLY FRIENDLY CONDITIONS AND STUDY OF ANTI-INFLAMMATORY AND ANTI-INFLAMMATORY AND ANTI-CARCINOGENIC ACTIVITIES IN BREAST CANCER.

• Grant number: 19/06201-4
• Support Opportunities: Regular Research Grants
• Start date: July 01, 2019
• End date: June 30, 2021
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Adriana Karla Cardoso Amorim Reis
• Grantee: Adriana Karla Cardoso Amorim Reis
• Host Institution: Instituto de Ciências Ambientais, Químicas e Farmacêuticas (ICAQF). Universidade Federal de São Paulo (UNIFESP). Campus Diadema. Diadema , SP, Brazil
• Associated researchers: Elaine Guadelupe Rodrigues ; Hugo Pequeno Monteiro

Abstract

The administration of non-steroidal anti-inflammatory drugs (NSAIDs) is one of the therapeutic resources most used in the treatment of acute or chronic processes associated with pain and / or inflammation and its efficacy is associated with inhibition of cyclooxygenase (COX) enzymes. The present project aims at the synthesis, under environmentally friendly conditions, of amides derived from NSAIDs, of the condensation reaction derivatives of these amides with cysteine and penicillamine, and of their S-nitrosothiols derived for the evaluation of COX-2 inhibitory activity by part of the various compounds synthesized. Recently, studies with NSAIDs in animal models have shown potential in the prevention of various types of cancer due to their ability to inhibit cyclooxygenase, which activity is correlated to several stages of oncogenesis. Cyclooxygenase (COX-2) isoform-2 inhibitors perform pleiotropic actions that may be useful in the treatment of breast cancer.This project aims at the synthesis, under environmentally friendly conditions, of amides derivativies of NSAIDs and the condensation reaction derivatives of these amides with cysteine and penicillamine, and of their S-nitrosothiols for the evaluation of COX-2 inhibitory activity by part of the various synthesized compounds.We also intend to establish correlations between the potential COX-2 inhibition capabilities of the synthesized compounds and their anti-inflammatory and anti-carcinogenic activities in vitro, against the MCF-10A, MDA-MB-231, MCF -7 and HUVEC. (AU)