Studies on duocarmycin SA and its derivatives.
New duocarmycin SA derivatives have been synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells, and in vivo antitumor activity against murine sarcoma 180 in mice. The results suggested that the N,N-dialkylcarbamoyl derivatives bearing the p-methoxy cinnamoyl group, which was prepared from duocarmycin SA, showed good in vivo antitumor activities superior to native duocarmycin SA.
Nagamura
S
S
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Asai
A
A
Kobayashi
E
E
Gomi
K
K
Saito
H
H
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000494:pharmacology; D018906:Antineoplastic Agents, Alkylating / Q000737:chemistry* / Q000494:pharmacology; D004355:Drug Stability; D000080890:Duocarmycins; D006367:HeLa Cells; D006801:Humans; D007211:Indoles; D051379:Mice; D008956:Models, Chemical; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D018906:Antineoplastic Agents, Alkylating; D000080890:Duocarmycins; D007211:Indoles; D011758:Pyrroles; C066098:duocarmycin SA