In:
Synthesis, Georg Thieme Verlag KG, Vol. 49, No. 18 ( 2017-09), p. 4335-4340
Abstract:
An efficient seven-step semisynthetic approach towards non-racemic bifunctional furano-allocolchicinoids, starting from naturally occurring colchicine is presented. The Pd-catalyzed domino Sonogashira coupling/5-endo-dig cyclization was employed as the key step. The prepared compounds exhibited substantial cytotoxicity against T3M4, MiaPaCa-2, Colo-357, and PANC-1 cell lines. The presence of two functionalities with different reactivity (hydroxyl and amino groups) in the target molecules allows for an easy conjugation of furano-allocolchicinoids with drug delivery carriers, and opens promising opportunities for their further exploitation in the search of therapeutics.
Type of Medium:
Online Resource
ISSN:
0039-7881
,
1437-210X
DOI:
10.1055/s-0036-1589060
Language:
English
Publisher:
Georg Thieme Verlag KG
Publication Date:
2017
detail.hit.zdb_id:
204080-3
detail.hit.zdb_id:
2033062-5
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