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ID: ALA1131966

Journal: Bioorg Med Chem Lett

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

Authors: LaCour TG, Guo C, Ma S, Jeong JU, Boyd MR, Matsunaga S, Fusetani N, Fuchs PL.

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.

CiteXplore: 10498214

DOI: 10.1016/s0960-894x(99)00430-8