✦ LIBER ✦

1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists

✍ Scribed by Jeffrey C. Kern; Eugene Terefenko; Eugene Trybulski; Thomas J. Berrodin; Jeffrey Cohen; Richard C. Winneker; Matthew R. Yudt; Zhiming Zhang; Yuan Zhu; Puwen Zhang

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 466 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.06.109

No coin nor oath required. For personal study only.

✦ Synopsis

Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase assay. Moderate to potent PR antagonists were achieved with these scaffolds. Several compounds (e.g., 15 and 20) demonstrated low nanomolar PR antagonist potency and good selectivity versus other steroid receptors.