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PubMed · 11374986

Target-directed enediynes: designed estramycins.

G B Jones·G Hynd·J M Wright·A Purohit·G W Plourde·R S Huber·J E Mathews·A Li·M W Kilgore·G J Bubley·M Yancisin·M A Brown
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Abstract

The goal of selective targeting of enediyne cytotoxins has been investigated using estrogenic delivery vehicles. A series of estrogen-enediyne conjugates were assembled, and affinity for human estrogen receptor [hERalpha] was determined. The most promising candidate induced receptor degradation following Bergman cycloaromatization and caused inhibition of estrogen-induced transcription in T47-D human breast cancer cells.

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AlkynesAntineoplastic Agents, HormonalBreast NeoplasmsCell DivisionCyclizationDrug Delivery SystemsEstradiol CongenersFemaleGene Expression Regulation, NeoplasticHumansReceptors, AndrogenReceptors, EstrogenTumor Cells, CulturedJournal ArticleResearch Support, U.S. Gov't, P.H.S.

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G B Jones, G Hynd, J M Wright, A Purohit, G W Plourde, R S Huber, J E Mathews, A Li, M W Kilgore, G J Bubley, M Yancisin, M A Brown. 2001-06-01. Target-directed enediynes: designed estramycins.. https://doi.org/10.1021/jo0055842

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