Title of article :
Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents
Author/Authors :
U Sharma، نويسنده , , J.C Marquis، نويسنده , , A. Nicole Dinaut، نويسنده , , S.M Hillier، نويسنده , , B Fedeles، نويسنده , , P.T Rye، نويسنده , , J.M Essigmann، نويسنده , , R.G Croy، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Abstract :
A series of bifunctional compounds was prepared consisting of 17β 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.
Keywords :
anti-cancer , Steroid–mustard conjugates , Breast cancer.* Corresponding authors. Tel.: +1-617-2536227 , fax: +1-617-2535445 , e-mail addresses: jessig@mit.edu , rgcroy@mit.edu
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters