2. Academic Validation
  3. On topography and functionality in the B-D rings of cephalostatin cytotoxins

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

Affiliation

  • 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.

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