1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5′-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 18, 2008, Pages 5015-5017

  Kern, Jeffrey C ^a   Terefenko, Eugene A ^a   Fensome, Andrew ^a   Unwalla, Ray ^a   Wrobel, Jay ^a   Cohen, Jeffrey ^a   Zhu, Yuan ^a   Berrodin, Thomas J ^a   Yudt, Matthew R ^a   Winneker, Richard C ^a   Zhang, Zhiming ^a   Zhang, Puwen ^a  

^a PFIZER INC   (United States)

Author keywords

Non steroidal; PR agonist; PR antagonist; Progesterone receptor (PR)

Indexed keywords

7 (5' CYANOPYRROL 2 YL)BENZO[1,4]OXAZEPIN 2 ONE DERIVATIVE; ALKALINE PHOSPHATASE; MIFEPRISTONE; PROGESTERONE; PROGESTERONE RECEPTOR MODULATOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BREAST CARCINOMA; CONTROLLED STUDY; DRUG ACTIVITY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ASSAY; HUMAN; HUMAN CELL; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

COMBINATORIAL CHEMISTRY TECHNIQUES; HUMANS; MOLECULAR STRUCTURE; OXAZEPINES; RECEPTORS, PROGESTERONE; STRUCTURE-ACTIVITY RELATIONSHIP;

HUMAN ECHOVIRUS 1;

EID: 51349151533     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.015     Document Type: Article

References (14)

1. Mangelsdorf D.J., Thummel C., Beato M., Herrlich P., Schuetz G., Umesono K., Blumberg B., Kastner P., and Mark M. Cell (Cambridge, Mass.) 83 (1995) 835
2. Yuzpe A.A. J. Reprod. Med. 47 (2002) 967
3. Brown A., Cheng L., Lin S., and Baird D.T. J. Clin. Endocrinol. Metabol. 87 (2002) 63
4. Kettel L.M., Murphy A.A., Morales A.J., and Yen S.S. Human Reprod. 9 Suppl. 1 (1994) 116
5. Kettel L.M., Murphy A.A., Morales A.J., and Yen S.S. Am. J. Obst. Gynecol. 178 (1998) 1151
6. Murphy A.A., Kettel L.M., Morales A.J., Roberts V.J., and Yen S.S. J. Clin. Endocrinol. Metabol. 76 (1993) 513
7. Murphy A.A., Morales A.J., Kettel L.M., and Yen S.S. Fertility Sterility 64 (1995) 187
8. Collins M.A., Hudak V., Bender R., Fensome A., Zhang P., Miller L., Winneker R.C., Zhang Z., Zhu Y., Cohen J., Unwalla R.J., and Wrobel J. Bioorg. Med. Chem. Lett. 14 (2004) 2185
9. Fensome A., Bender R., Chopra R., Cohen J., Collins M.A., Hudak V., Malakian K., Lockhead S., Olland A., Svenson K., Terefenko E.A., Unwalla R.J., Wilhelm J.M., Wolfrom S., Zhu Y., Zhang Z., Zhang P., Winneker R.C., and Wrobel J. J. Med. Chem. 48 (2005) 5092
10. Zhang P., Terefenko E.A., Fensome A., Wrobel J., Winneker R., Lundeen S., Marschke K.B., and Zhang Z. J. Med. Chem. 45 (2002) 4379
11. For separate work on the 7-phenyl based 1,5-dihydrobenzo[e][1,4]oxazepin-2-ones, see Ref.:. Zhang P., Kern J.C., Terefenko E.A., Fensome A., Unwalla R., Zhang Z., Cohen J., Berrodin T.J., Yudt M.R., Winneker R.C., and Wrobel J. Bioorg. Med. Chem. 16 (2008) 6589
12. Fensome A., Adams W.R., Adams A.L., Berrodin T.J., Cohen J., Huselton C., Illenberger A., Kern J.C., Hudak V.A., Marella M.A., Melenski E.G., McComas C.C., Mugford C.A., Slayden O.D., Yudt M., Zhang Z., Zhang P., Zhu Y., Winneker R.C., and Wrobel J.E. J. Med. Chem. 51 (2008) 1861
13. Terefenko E.A., Kern J., Fensome A., Wrobel J., Zhu Y., Cohen J., Winneker R., Zhang Z., and Zhang P. Bioorg. Med. Chem. Lett. 15 (2005) 3600
14. Sadowski I., Bell B., Broad P., and Hollis M. Gene 118 (1992) 137