Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues.
A series of novel cyclic analogues of curcumin were synthesized and analyzed for in vitro cytostatic activity. Condensation of 2-acetylcycloalkanones with a variety of aromatic aldehydes resulted in the formation of 2-arylidene-6-(3-arylacryoyl)-cycloalkanone derivatives. A number of these analogues were found to have significant anticancer activity against representative murine and human cancer cell lines during in vitro bioassays. This corroborated with in vitro cytostatic activity against a panel of 60 cell lines studied at the National Cancer Institute (USA).
Youssef
Dani
D
Département des Sciences, Université Sainte-Anne, Church Point, NS, Canada B0W 1M0.
Nichols
Christie E
CE
Cameron
T Stanley
TS
Balzarini
Jan
J
De Clercq
Erik
E
Jha
Amitabh
A
D000818:Animals; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D003474:Curcumin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D054697:Cytostatic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity*; D015195:Drug Design; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D054697:Cytostatic Agents; D003474:Curcumin