Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.
In the course of a study of 6-N-amino-substituted analogues of NB-506 (1), a more potent anticancer drug, J-109,404 (2), in which the formyl group of NB-506 was replaced with a 1,3-dihydroxypropane group, was reported. A study of further modification in the positions of two hydroxyl groups at the indole rings of 2 resulted in the discovery of a 2,10-dihydroxy analogue, J-107,088 (3), which is a promising anticancer agent with a broader therapeutic window than J-109,404.
Ohkubo
M
M
Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories, Ibaraki, Japan.
Nishimura
T
T
Honma
T
T
Nishimura
I
I
Ito
S
S
Yoshinari
T
T
Suda
H A
HA
Morishima
H
H
Nishimura
S
S
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002227:Carbazoles; D005960:Glucosides; C092476:NB 506