On topography and functionality in the B-D rings of cephalostatin cytotoxins.
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.
LaCour
T G
TG
Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Guo
C
C
Ma
S
S
Jeong
J U
JU
Boyd
M R
MR
Matsunaga
S
S
Fusetani
N
N
Fuchs
P L
PL
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents