Preparation of new alkyne-modified ansamitocins by mutasynthesis
The preparation of alkyne-modified ansamitocins by mutasynthetic supplementation of Actinosynnema pretiosum mutants with alkyne-substituted aminobenzoic acids is described. This modification paved the way to introduce a thiol linker by Huisgen-type cycloaddition which can principally be utilized to create tumor targeting conjugates. In bioactivity tests, only those new ansamitocin derivatives showed strong antiproliferative activity that bear an ester side chain at C-3.
Harmrolfs, Kirsten,Mancuso, Lena,Drung, Binia,Sasse, Florenz,Kirschning, Andreas
supporting information
p. 535 - 543
(2014/04/17)
BENZAMIDE DERIVATIVE WITH ANTICANCER ACTIVITY AND PREPARATION METHOD AND USE THEREOF
Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out
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(2013/09/12)
INDOLOYLGUANIDINE DERIVATIVES
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(2008/06/13)
6-SUBSTITUTED INDOLES FROM o-HALONITROBENZENES
o-Chloro- and o-bromonitrobenzenes are efficiently converted to 6-substituted indoles in a four step synthesis, proceeding through o-trimethylsilylethynylnitrobenzenes, o-nitrophenylacetaldehyde dimethylacetals and o-aminophenylacetaldehyde dimethylacetal
Tischler, Allan N.,Lanza, Thomas J.
p. 1653 - 1656
(2007/10/02)
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