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

Analogues 12′β-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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2587-2592
Main Authors: LaCour, Thomas G., Guo, Chuangxing, Ma, Sunghoon, Jeong, Jae Uk, Boyd, Michael R., Matsunaga, Shikegi, Fusetani, Nobuhiro, Fuchs, P.L.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
General aspects
Humans
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Tumor Cells, Cultured
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Summary:Analogues 12′β-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00430-8