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Design and synthesis of azaisoflavone analogs as phytoestrogen mimetics
- Gim, Hyo Jin;
- Li, Hua;
- Jung, So Ra;
- Park, Yong Joo;
- Ryu, Jae-Ha;
- ... Jeon, Raok;
- 외 1명
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16초록
A series of azaisoflavone analogs were designed and synthesized and their transactivation activities and binding affinities for ER alpha and ER beta were investigated. Among these compounds, 2b and 3a were the most potent with 6.5 and 1.1 mu M of EC50, respectively. Molecular modeling study showed putative binding modes of the compound 3a in the active site of ER alpha and ER beta, which were similar with that of genistein and provided insight of the effect of N-alkyl substitution of azaisoflavones on ER beta activity. Also, a biphasic effect of azaisoflavone analogs on MCF-7 cell growth depending on their concentrations was investigated. (C) 2014 Elsevier Masson SAS. All rights reserved.
키워드
Estrogen receptor; ER agonist; Azaisoflavones; Proliferation; ESTROGEN-RECEPTOR-BETA; BREAST-CANCER CELLS; HEALTHY POSTMENOPAUSAL WOMEN; IN-VITRO; TYROSINE KINASE; PLUS PROGESTIN; ER-ALPHA; GENISTEIN; GROWTH; PROLIFERATION
- 제목
- Design and synthesis of azaisoflavone analogs as phytoestrogen mimetics
- 저자
- Gim, Hyo Jin; Li, Hua; Jung, So Ra; Park, Yong Joo; Ryu, Jae-Ha; Chung, Kyu Hyuck; Jeon, Raok
- 발행일
- 2014-10
- 유형
- Article
- 권
- 85
- 페이지
- 107 ~ 118