Structure-activity relationship of a novel antitumor ansamycin antibiotic trienomycin A and related compounds.
Various derivatives of trienomycin A (1) were prepared and tested for cytocidal activities. All the derivatives except for 22-O-methyltrienomycin A (5) showed reduced cytotoxicity compared with 1. It is concluded that the existence of a triene moiety, free 13-OH and an acyl group at C-11 owe important role for cytocidal activity.
Funayama
S
S
Kitasato Institute, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Anraku
Y
Y
Mita
A
A
Yang
Z B
ZB
Shibata
K
K
Komiyama
K
K
Umezawa
I
I
Omura
S
S
D000409:Alanine / Q000031:analogs & derivatives; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006367:HeLa Cells / Q000187:drug effects; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D013329:Structure-Activity Relationship
D000903:Antibiotics, Antineoplastic; D003509:Cyclohexanecarboxylic Acids; C045958:trienomycin A; D000409:Alanine