Synthesis and anticancer activities of ageladine A and structural analogs.
A series of ageladine A analogs that include 2-aminoimidazo[4,5-c]azepines (seven-membered rings) and 2-amino-3H-imidazo[4,5-c]pyridine (six-membered rings) derivatives were synthesized and evaluated for their anticancer effects against several human cancer cell lines and MMP-2 inhibition in vitro. Only compounds possessing the aromatic azepine (seven-membered ring) core showed anticancer activity with IC(50) values in the low micromolar range.
Ma
Yuelong
Y
Department of Molecular Medicine, Beckman Research Institute at City of Hope, Duarte, CA 91010, United States.
Nam
Sangkil
S
Jove
Richard
R
Yakushijin
Kenichi
K
Horne
David A
DA
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D061965:Matrix Metalloproteinase Inhibitors; D010084:Oxidation-Reduction; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
C482289:Ageladine A; D000970:Antineoplastic Agents; D007093:Imidazoles; D061965:Matrix Metalloproteinase Inhibitors; D011758:Pyrroles; C014973:2-aminoimidazole; D020778:Matrix Metalloproteinase 2; C077209:oroidin