2. Academic Validation
  3. Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies

  • Bioorg Med Chem Lett. 2007 Oct 15;17(20):5563-6. doi: 10.1016/j.bmcl.2007.08.009.
Timothy I Richardson 1,  Jeffrey A Dodge,  Yong Wang,  Jim D Durbin,  Venkatesh Krishnan,  Bryan H Norman
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. t_richardson@lilly.com
PMID: 17804226 DOI: 10.1016/j.bmcl.2007.08.009
Abstract

Benzopyrans are selective Estrogen Receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the synthesis of a late stage intermediate that allowed us to combine A-ring and C-ring modifications and carry out simultaneous SAR studies at both positions. Modification of both positions proved additive, maintaining affinity and improving ERbeta selectivity up to 83-fold. An X-ray cocrystal structure confirms the previously observed binding mode in ERbeta.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z