Arzneimittelforschung 2002; 52(1): 39-44
DOI: 10.1055/s-0031-1299854
Sex Hormones and Inhibitors
Editio Cantor Verlag Aulendorf (Germany)

Synthesis of Some New Diaryl and Triaryl Hydrazone Derivatives as Possible Estrogen Receptor Modulators

Jaya Pandey
a   Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India
,
Rekha Pal
b   Endocrinology Division, Central Drug Research Institute, Lucknow, India
,
Anila Dwivedi
b   Endocrinology Division, Central Drug Research Institute, Lucknow, India
,
Kanchan Hajela
a   Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India
› Author Affiliations
Further Information

Publication History

Publication Date:
26 December 2011 (online)

Summary

l,2-Bis(4-substituted phenyl)-2-methyl ethanone (2,4-dlnitrophenyl)hydrazones and 1-naphthyl-1-(4-substituted phenyl)-methanone (2,4-dinitrophenyl)hydrazones have been synthesized and evaluated for their anti-implantation, uterotrophic, antiuterotrophic, anticancer and antimicrobial activities. Diphenolic hy-drazone (compound 6) showed maximum uterotrophic inhibition of 70 %, whereas compound 20 exhibited cytotoxicity in the range of 50–70 % against MCF-7 and ZR-75-1 human malignant breast cell lines.

Zusammenfassung

Synthese neuer Diaryl- und Triarylhydrazon-Derivate als potentielle Modulatoren von Estrogen-Rezeptoren

l,2-Bis(4-substituierte phenyl)-2-methylethanon(2,4-dinitrophenyl)hydrazone und 1-Naphthyl-1-(4-substituierte) methanon(2,4-dinitrophenyl)hydrazone wurden synthetisiert und auf Anti-Implantations-, uterotrophe, antiuterotrophe, krebshemmende und antimikro-bielle Wirkungen geprüft. Diphenolisches Hydrazon (Verbindung 6) zeigte maximale uterotrophe Hemmung von 70 %, während Verbindung 20 bei menschlichen malignen MCF-7- und ZR-75-1-Brustzellinien zytostatische Aktivität von 50–70 % aufwies.