title: Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.
abstract: 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.
authors.affiliation: Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories, Ibaraki, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Ohkubo
authors.forename: T
authors.initials: T
authors.lastname: Nishimura
authors.forename: T
authors.initials: T
authors.lastname: Honma
authors.forename: I
authors.initials: I
authors.lastname: Nishimura
authors.forename: S
authors.initials: S
authors.lastname: Ito
authors.forename: T
authors.initials: T
authors.lastname: Yoshinari
authors.forename: H A
authors.initials: HA
authors.lastname: Suda
authors.forename: H
authors.initials: H
authors.lastname: Morishima
authors.forename: S
authors.initials: S
authors.lastname: Nishimura
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles; D005960:Glucosides; C092476:NB 506