2. Academic Validation
  3. Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism

Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism

  • Bioorg Med Chem Lett. 2016 Apr 1;26(7):1844-8. doi: 10.1016/j.bmcl.2016.01.089.
Taelim Kim 1,  Hye-In Kim 2,  Ji-Young An 1,  Jun Lee 1,  Na-Rae Lee 2,  Jinyuk Heo 1,  Ji-Eun Kim 2,  Jihyun Yu 1,  Yong Sup Lee 1,  Kyung-Soo Inn 3,  Nam-Jung Kim 4
Affiliations

Affiliations

  • 1 Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
  • 2 Department of Pharmaceutical Science, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
  • 3 Department of Pharmaceutical Science, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: innks@khu.ac.kr.
  • 4 Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: kimnj@khu.ac.kr.
PMID: 26905830 DOI: 10.1016/j.bmcl.2016.01.089
Abstract

In this study, a series of bis(4-hydroxy)benzophenone oxime ether derivatives such as 12c, 12e and 12h were identified as novel Estrogen Receptor (ER) agonists that have additional and complementary anti-proliferative activities via ER-independent mechanism in Cancer cells. These compounds are expected to overcome the therapeutic limitation of existing ER agonists such as estradiol and tamoxifen, which have been known to induce the proliferation of Cancer cells.

Keywords

Anti-cancer activities; Bisphenol; Complementary; Estrogen receptor (ER) agonists; Oxime ether.

Figures