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

doi:10.1021/jo0055842

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

Pharmacology and Nutritional Sciences

Research output: Contribution to journal › Article › peer-review

62 Scopus citations

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 [hERα] 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.

Original language	English
Pages (from-to)	3688-3695
Number of pages	8
Journal	Journal of Organic Chemistry
Volume	66
Issue number	11
DOIs	https://doi.org/10.1021/jo0055842
State	Published - Jun 1 2001

Funding

Funders	Funder number
National Institute of General Medical Sciences	R01GM057123

ASJC Scopus subject areas

Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1021/jo0055842

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title = "Target-directed enediynes: Designed estramycins",

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 [hERα] 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.",

author = "Jones, \{G. B.\} and G. Hynd and Wright, \{J. M.\} and A. Purohit and Plourde, \{G. W.\} and Huber, \{R. S.\} and Mathews, \{J. E.\} and A. Li and Kilgore, \{M. W.\} and Bubley, \{G. J.\} and M. Yancisin and Brown, \{M. A.\}",

year = "2001",

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doi = "10.1021/jo0055842",

language = "English",

volume = "66",

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T1 - Target-directed enediynes

T2 - Designed estramycins

AU - Jones, G. B.

AU - Hynd, G.

AU - Wright, J. M.

AU - Purohit, A.

AU - Plourde, G. W.

AU - Huber, R. S.

AU - Mathews, J. E.

AU - Li, A.

AU - Kilgore, M. W.

AU - Bubley, G. J.

AU - Yancisin, M.

AU - Brown, M. A.

PY - 2001/6/1

Y1 - 2001/6/1

N2 - 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 [hERα] 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.

AB - 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 [hERα] 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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U2 - 10.1021/jo0055842

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AN - SCOPUS:0035356676

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VL - 66

SP - 3688

EP - 3695

JO - Journal of Organic Chemistry

JF - Journal of Organic Chemistry

IS - 11

ER -

Target-directed enediynes: Designed estramycins

Abstract

Funding

ASJC Scopus subject areas

UN SDGs

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