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

63 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

UN SDGs

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

SDG 3 Good Health and Well-being

ASJC Scopus subject areas

Organic Chemistry

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10.1021/jo0055842

Cite this

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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",

month = jun,

day = "1",

doi = "10.1021/jo0055842",

language = "English",

volume = "66",

pages = "3688--3695",

number = "11",

}

TY - JOUR

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.

UR - https://www.scopus.com/pages/publications/0035356676

UR - https://www.scopus.com/pages/publications/0035356676#tab=citedBy

U2 - 10.1021/jo0055842

DO - 10.1021/jo0055842

M3 - Article

C2 - 11374986

AN - SCOPUS:0035356676

SN - 0022-3263

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

UN SDGs

ASJC Scopus subject areas

Access to Document

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