Sloan-kettering Institute for Cancer Research

Christopher Borella

David A Scheinberg

Francis M Sirotnak

William G Bornmann

Howard Scher

Ephraim Vidal

The present invention provides methods for the asymmetric synthesis of (S,S,R)-(&#x2212;)-actinonin and its analogs and the compounds thereby synthesized having a structural formula:where Ris an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said Rfurther comprising a cyclic or bicyclic structure; Ris methyl, CHCH, (CH)CH, C(CH), phenyl, 3,4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH-(N-Boc-4-piperidine), 4-tetrahydropyran, CH-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; Ris Ror Calkyl, Ris Calkyl; and Ris NH, OH, NHOH, NHOCH, N(CH)OH, N(CH)OCH, NHCHCH, NH(CHCH), NHCH(2,4-(OCH3)Ph, NHCH(4-NO)Ph, NHN(CH), proline, or 2-hydroxymethyl pyrrolidine. Additionally, a method for the treatment of a neoplastic disease or for the inhibition of tumor cell growth each comprising the step of administering to an individual in need of such treatment a pharmacologically effective dose of the compounds of the present invention are provided.

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Christopher Borella