| 摘要 |
The present invention provides methods for the asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R<SUP>1 </SUP>is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R<SUP>1 </SUP>further comprising a cyclic or bicyclic structure; R<SUP>2 </SUP>is methyl, CH<SUB>2</SUB>CH<SUB>3</SUB>, (CH<SUB>2</SUB>)<SUB>2</SUB>CH<SUB>3</SUB>, C(CH<SUB>3</SUB>)<SUB>3</SUB>, phenyl, 3,4-dichlorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH<SUB>2</SUB>-(N-Boc-4-piperidine), 4-tetrahydropyran, CH<SUB>2</SUB>-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R<SUP>3 </SUP>is R<SUP>2 </SUP>or C<SUB>3-8</SUB>alkyl, R<SUP>4 </SUP>is C<SUB>1-3</SUB>alkyl; and R<SUP>5 </SUP>is NH<SUB>2</SUB>, OH, NHOH, NHOCH<SUB>3</SUB>, N(CH<SUB>3</SUB>)OH, N(CH<SUB>3</SUB>)OCH<SUB>3</SUB>, NHCH<SUB>2</SUB>CH<SUB>3</SUB>, NH(CH<SUB>2</SUB>CH<SUB>3</SUB>), NHCH<SUB>2</SUB>(2,4-(OCH3)<SUB>2</SUB>Ph, NHCH<SUB>2</SUB>(4-NO<SUB>2</SUB>)Ph, NHN(CH<SUB>3</SUB>)<SUB>2</SUB>, 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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