Drug intelligence / Profile preview

3-indomethacinoxyiminoolean-en-28-oic acid benzyl ester

Development stage
Preclinical
Lead developer
Poznan University of Medical Sciences
Modality
Small Molecules
01

Overview

3-indomethacinoxyiminoolean-en-28-oic acid benzyl ester is a synthetic small molecule conjugate consisting of the nonsteroidal anti-inflammatory drug (NSAID) indomethacin and an oleanolic acid oxime (OAO) derivative. Developed by researchers at the Poznan University of Medical Sciences, this compound is designed to synergize the anti-inflammatory and anti-tumorigenic effects of triterpenoids and NSAIDs while potentially mitigating the side effects associated with long-term NSAID use. The molecule acts as a dual modulator of the Nrf2-ARE and NF-κB signaling pathways. In pancreatic cancer cell models (PSN-1), it has been shown to decrease the nuclear translocation and DNA binding of Nrf2 and NF-κB subunits (p50 and p65), leading to the reduced expression of downstream proteins such as superoxide dismutase 1 (SOD-1) and cyclooxygenase-2 (COX-2). By inhibiting these pathways, the conjugate may overcome chemoresistance and serve as a potential therapeutic or chemopreventive agent for pancreatic cancer and hepatocellular carcinoma.

Other names
3-indomethacinoxyiminoolean-12-en-28-oic acid benzyl esterOAO-IND benzyl ester conjugate
02

Targets

Misfolded SOD1NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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