On topography and functionality in the B-D rings of cephalostatin cytotoxins

  • Bioorg Med Chem Lett. 1999 Sep 6;9(17):2587-92. doi: 10.1016/s0960-894x(99)00430-8.
T G LaCour  1 ,  C Guo ,  S Ma ,  J U Jeong ,  M R Boyd ,  S Matsunaga ,  N Fusetani ,  P L Fuchs
Affiliations
  • 1. Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
PMID: 10498214 DOI: 10.1016/s0960-894x(99)00430-8
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.