title: On topography and functionality in the B-D rings of cephalostatin cytotoxins.
abstract: Analogues 12'beta-hydroxycephalostatin 1 (9), 7'-deoxyritterazine G (10), and 14-epi-7'-deoxyritterazine B (11) were prepared via our protocol for unsymmetrical pyrazine synthesis. Cytotoxicity against human tumors was also determined for the first time for ritterazines, with femtomolar potency and a high correlation to cephalostatins observed. The SAR of these and related compounds provide insight into the importance of topography and certain chemical functionality in the B-D and B'-D' rings of cephalostatin type antineoplastics.
authors.affiliation: Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
authors.forename: T G
authors.initials: TG
authors.lastname: LaCour
authors.forename: C
authors.initials: C
authors.lastname: Guo
authors.forename: S
authors.initials: S
authors.lastname: Ma
authors.forename: J U
authors.initials: JU
authors.lastname: Jeong
authors.forename: M R
authors.initials: MR
authors.lastname: Boyd
authors.forename: S
authors.initials: S
authors.lastname: Matsunaga
authors.forename: N
authors.initials: N
authors.lastname: Fusetani
authors.forename: P L
authors.initials: PL
authors.lastname: Fuchs
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents