Synthesis of some new diaryl and triaryl hydrazone derivatives as possible estrogen receptor modulators.
1,2-Bis(4-substituted phenyl)-2-methyl ethanone (2,4-dinitrophenyl)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 hydrazone (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.
Pandey
Jaya
J
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India.
Pal
Rekha
R
Dwivedi
Anila
A
Hajela
Kanchan
K
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D010064:Embryo Implantation / Q000187:drug effects; D004965:Estrogen Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D008826:Microbial Sensitivity Tests; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014590:Uterine Contraction / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D004965:Estrogen Antagonists; D006835:Hydrazones; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators