Synthesis and antitumor activity of leinamycin derivatives: modifications of C-8 hydroxy and C-9 keto groups.
A series of leinamycin derivatives were synthesized and evaluated for antitumor activity. Modifications at C-8 and C-9 positions revealed a broad structure-activity relationship in vitro and some derivatives showed potent antiproliferative activity against HeLa S3 cells.
Kanda
Y
Y
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Ashizawa
T
T
Saitoh
Y
Y
Saito
H
H
Gomi
K
K
Okabe
M
M
D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D002455:Cell Division / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D007202:Indicators and Reagents; D007769:Lactams; D018942:Macrolides; D008968:Molecular Conformation; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles; D013871:Thiones
D000903:Antibiotics, Antineoplastic; D007202:Indicators and Reagents; D007769:Lactams; D018942:Macrolides; D013844:Thiazoles; D013871:Thiones; C059000:leinamycin