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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; Chung, Kyu Hyuck; Jeon, Raok.
Affiliation
  • Gim HJ; Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea.
  • Li H; Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea.
  • Jung SR; Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea.
  • Park YJ; School of Pharmacy, Sungkyunkwan University, 2066, Seobu-ro, Jangan-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
  • Ryu JH; Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea.
  • Chung KH; School of Pharmacy, Sungkyunkwan University, 2066, Seobu-ro, Jangan-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
  • Jeon R; Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea. Electronic address: rjeon@sookmyung.ac.kr.
Eur J Med Chem ; 85: 107-18, 2014 Oct 06.
Article in En | MEDLINE | ID: mdl-25078314
ABSTRACT
A series of azaisoflavone analogs were designed and synthesized and their transactivation activities and binding affinities for ERα and ERß were investigated. Among these compounds, 2b and 3a were the most potent with 6.5 and 1.1 µM of EC50, respectively. Molecular modeling study showed putative binding modes of the compound 3a in the active site of ERα and ERß, which were similar with that of genistein and provided insight of the effect of N-alkyl substitution of azaisoflavones on ERß activity. Also, a biphasic effect of azaisoflavone analogs on MCF-7 cell growth depending on their concentrations was investigated.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Drug Design / Quinolones / Flavones / Phytoestrogens Limits: Humans Language: En Journal: Eur J Med Chem Year: 2014 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Drug Design / Quinolones / Flavones / Phytoestrogens Limits: Humans Language: En Journal: Eur J Med Chem Year: 2014 Document type: Article