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Synthesis of C-1 homologues of pancratistatin and their preliminary biological evaluation.

Abstract：

:The synthesis of two C-1 analogues of pancratistatin has been accomplished in 17 steps from bromobenzene. The key steps involved the enzymatic dihydroxylation, regioselective opening of epoxyaziridine 9 with the alane derived from 8, a solid-state silica-gel-catalyzed intramolecular opening of aziridine to produce phenanthrene 13 whose oxidative cleavage and recyclization provided the full skeleton of the Amaryllidaceae constituents. The new analogues 5 and 6 exhibited promising activity in several human cancer cell lines.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Vshyvenko S,Scattolon J,Hudlicky T,Romero AE,Kornienko A

doi

10.1016/j.bmcl.2011.06.068

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4750-2

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00851-1

journal_volume

21

pub_type

杂志文章

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