Side chain modifications of (indol-3-yl)glyoxamides as antitumor agents.
New series of analogues of N-(pyridin-4-yl)-2-[1-(4-chlorobenzyl)-indol-3-yl]glyoxamide D-24851 were synthesized, characterized and tested for their in vitro anticancer properties. In the first series, an amino acid spacer was introduced in the glyoxamide chain of D-24851. In the second series, the glyoxamide chain was moved to positions 4 and 5 of indole skeleton. These new compounds were tested on four cancer cell lines (KB, SK-OV-3, NCI-H460 and SF-268), with promising activity for the glycine derivative.
Antoine
Maud
M
Département de Pharmacochimie, Faculté de Pharmacie, Nantes Université, Nantes, France.
Marchand
Pascal
P
Le Baut
Guillaume
G
Czech
Michael
M
Baasner
Silke
S
Gunther
Eckhard
E
D000081:Acetamides / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D005998:Glycine; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000081:Acetamides; D000970:Antineoplastic Agents; D007211:Indoles; C419187:indibulin; D005998:Glycine