Drug intelligence / Profile preview

prodigiosene-estrone conjugate 3c

Development stage
Preclinical
Lead developer
Dalhousie University
Modality
Small Molecules
Administration
Parenteral
01

Overview

Prodigiosene-estrone conjugate 3c is a research-stage small molecule hybrid compound consisting of a synthetic prodigiosene (a prodigiosin analogue) covalently conjugated to estrone via an 8-carbon ester linker. Developed by Alison Thompson's group at Dalhousie University, this first-generation conjugate was designed to target estrogen receptor-positive (ER+) breast cancer cells with greater selectivity than prodigiosin alone. The estrone moiety acts as a targeting ligand to direct the cytotoxic tripyrrolic prodigiosene scaffold to the estrogen receptor (ER). In biological testing against the MCF-7 breast cancer cell line, compound 3c exhibited modest antiproliferative activity but performed relatively poorly compared to shorter-chain analogues (3a and 3b), likely due to the high sensitivity of its ester linkage to hydrolysis, which limits its stability.

Other names
compound 3ccompound3ccompound-3cprodigiosene-estrone conjugate 3c
02

Targets

ER (Estrogen receptor)DNA

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