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On topography and functionality in the B-D rings of cephalostatin cytotoxins
T G LaCour1, C Guo, S Ma
1Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Bioorganic & Medicinal Chemistry Letters
|September 25, 1999
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.