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Drug intelligence / Profile preview
prodigiosene-4-hydroxytamoxifen conjugate 4c
- Development stage
- Preclinical
- Lead developer
- Dalhousie University
- Modality
- Small Molecules
- Administration
- Parenteral
01
Overview
prodigiosene-4-hydroxytamoxifen conjugate 4c is a synthetic small molecule conjugate consisting of a tripyrrolic prodigiosene pharmacophore linked to a 4-hydroxytamoxifen (afimoxifene) targeting moiety via an ester linker. Developed by researchers at Dalhousie University, this conjugate is designed to selectively target estrogen receptor (ER)-positive breast cancer cells, such as the MCF-7 cell line. The 4-hydroxytamoxifen component binds to the estrogen receptor, facilitating cellular uptake, while the prodigiosene component acts as a transmembrane anion transporter, disrupting intracellular pH, inducing apoptosis, and exhibiting nanomolar-range antiproliferative activity.
- Other names
- prodigiosene-4-hydroxytamoxifen conjugate 4cprodigiosene4-hydroxytamoxifen conjugate 4cprodigiosene 4-hydroxytamoxifen conjugate 4cprodigiosene-tamoxifen conjugate 4c
02
Targets
ESR1 (ERα)ESR2 (ERβ)
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