Premium
Novel Piperidinedione Analogs as Inhibitors of Breast Cancer Cell Growth
Author(s) -
AbouZeid A.,
ElMowafy A. M.,
ElAshmawy M. B.,
Hendry L. B.,
Abdelal A. M.,
Badria F. A.
Publication year - 2000
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(200012)333:12<431::aid-ardp431>3.0.co;2-m
Subject(s) - breast cancer , tamoxifen , mcf 7 , human breast , cancer cell , cancer , chemistry , cell growth , cancer cell lines , biological activity , cancer research , pharmacology , endogeny , dna synthesis , cell culture , dna , biochemistry , biology , medicine , in vitro , genetics
We previously reported the utility of antineoplaston‐A10 (3‐phenylacetylamino‐2,6‐piperidinedione) as an endogenous cancer protector and immune modulator in breast cancer patients ( Cancer Lett ., 2000 , 157, 57 ). In this study, four new piperidinedione A10 analogs were synthesized and tested for their antimitotic activity on a human breast cancer cell line against the prototype A10 and the antibreast cancer drug tamoxifen. Moreover, the DNA binding capacity of such compounds was evaluated against A10. ( E )‐3‐(4‐Nitrocinnamoylamino)‐2,6‐piperidinedione “ 3B ” and ( E )‐3‐(4‐hydroxycinnamoylamino)‐2,6‐piperidinedione “ 3D ” were several‐fold more potent antiproliferative agents than A10 and tamoxifen. They also had significantly higher capacity to bind DNA than A10. Conversely, (E)‐3‐(cinnamoylamino)‐2,6‐piperidinedione “ 3A ” and ( E )‐3‐(4‐methoxycinnamoylamino)‐2,6‐piperidinedione) “ 3C ” had weaker biological profiles than the lead compound A10. Detailed synthetic, spectroscopic, and biological data are reported.