Drug intelligence / Profile preview

prodigiosene-estrone conjugate 3b

Development stage
Preclinical
Lead developer
Dalhousie University
Modality
Small Molecules
01

Overview

prodigiosene-estrone conjugate 3b is a research-stage small molecule anticancer conjugate consisting of a synthetic prodigiosene (a prodigiosin analogue) covalently linked to estrone via a 4-carbon (n=4) ester linker. Developed at Dalhousie University, the compound was designed to target estrogen receptor-positive (ER+) breast cancer cells by utilizing the estrone moiety as a targeting vector to deliver the cytotoxic prodigiosene payload selectively. In vitro studies in MCF-7 breast cancer cells demonstrated that the conjugate reduces cell viability without inducing the estrogenic proliferative effects associated with estrone alone, suggesting its mechanism of action is driven primarily by the cytotoxic effects of the prodigiosene pharmacophore rather than estrogen receptor activation. It remains a purely academic research tool with no commercial development or approved brand names.

Other names
3b
02

Targets

ESR1 (ERα)V-ATPase (Vacuolar-type H+-ATPase)TOP1 (DNA Topoisomerase I)TOP2A (DNA topoisomerase II)ESR2 (ERβ)DNA

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