Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents

U Sharma; J C Marquis; A Nicole Dinaut; S M Hillier; B Fedeles; P T Rye; J M Essigmann; R G Croy

doi:10.1016/j.bmcl.2004.04.064

Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents

U Sharma, J C Marquis, A Nicole Dinaut, S M Hillier, B Fedeles, P T Rye, J M Essigmann, R G Croy

Deanery of Clinical Sciences

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

Abstract / Description of output

A series of bifunctional compounds was prepared consisting of 17beta estradiol linked to a DNA damaging N,N-bis-(2-chloroethyl)aniline. The objective of our studies was to determine the characteristics of the linker that permitted both reaction with DNA and binding of the resultant covalent adducts to the estrogen receptor. Linker characteristics were pivotal determinants underlying the ability of the compounds to kill selectively breast cancer cells that express the estrogen receptor.

Original language	English
Pages (from-to)	3829-33
Number of pages	5
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	14
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2004.04.064
Publication status	Published - 2004

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10.1016/j.bmcl.2004.04.064

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title = "Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents",

abstract = "A series of bifunctional compounds was prepared consisting of 17beta estradiol linked to a DNA damaging N,N-bis-(2-chloroethyl)aniline. The objective of our studies was to determine the characteristics of the linker that permitted both reaction with DNA and binding of the resultant covalent adducts to the estrogen receptor. Linker characteristics were pivotal determinants underlying the ability of the compounds to kill selectively breast cancer cells that express the estrogen receptor.",

author = "U Sharma and Marquis, {J C} and {Nicole Dinaut}, A and Hillier, {S M} and B Fedeles and Rye, {P T} and Essigmann, {J M} and Croy, {R G}",

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AU - Sharma, U

AU - Marquis, J C

AU - Nicole Dinaut, A

AU - Hillier, S M

AU - Fedeles, B

AU - Rye, P T

AU - Essigmann, J M

AU - Croy, R G

PY - 2004

Y1 - 2004

N2 - A series of bifunctional compounds was prepared consisting of 17beta estradiol linked to a DNA damaging N,N-bis-(2-chloroethyl)aniline. The objective of our studies was to determine the characteristics of the linker that permitted both reaction with DNA and binding of the resultant covalent adducts to the estrogen receptor. Linker characteristics were pivotal determinants underlying the ability of the compounds to kill selectively breast cancer cells that express the estrogen receptor.

AB - A series of bifunctional compounds was prepared consisting of 17beta estradiol linked to a DNA damaging N,N-bis-(2-chloroethyl)aniline. The objective of our studies was to determine the characteristics of the linker that permitted both reaction with DNA and binding of the resultant covalent adducts to the estrogen receptor. Linker characteristics were pivotal determinants underlying the ability of the compounds to kill selectively breast cancer cells that express the estrogen receptor.

U2 - 10.1016/j.bmcl.2004.04.064

DO - 10.1016/j.bmcl.2004.04.064

M3 - Article

C2 - 15203171

SN - 0960-894X

VL - 14

SP - 3829

EP - 3833

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 14

ER -

Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents

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