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Nitrosopurines en route to potently cytotoxic asmarines.


ABSTRACT: A nitrosopurine ene reaction easily assembles the asmarine pharmacophore and transmits remote stereochemistry to the diazepine-purine hetereocycle. This reaction generates potent cytotoxins which exceed the potency of asmarine?A (1.2??M IC50) and supersede the metabolites as useful leads for biological discovery.

SUBMITTER: Wan KK 

PROVIDER: S-EPMC4470469 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature

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Nitrosopurines en route to potently cytotoxic asmarines.

Wan Kanny K KK   Iwasaki Kotaro K   Umotoy Jeffrey C JC   Wolan Dennis W DW   Shenvi Ryan A RA  

Angewandte Chemie (International ed. in English) 20150107 8


A nitrosopurine ene reaction easily assembles the asmarine pharmacophore and transmits remote stereochemistry to the diazepine-purine hetereocycle. This reaction generates potent cytotoxins which exceed the potency of asmarine A (1.2 μM IC50) and supersede the metabolites as useful leads for biological discovery. ...[more]

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