当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > The new facile and straightforward method for the synthesis of 4H-1,2,3-thiadiazolo[5,4-b]indoles and determination of their antiproliferative activity.

The new facile and straightforward method for the synthesis of 4H-1,2,3-thiadiazolo[5,4-b]indoles and determination of their antiproliferative activity.

Abstract：

:A series of 4H-1,2,3-thiadiazolo[5,4-b]indoles were synthesized by novel tandem of oxidative cyclization of 3-alkoxycarbonylhydrazonoindoline-2-thiones, 1,5-H-shift and elimination of tert-butoxy(ethoxy)carbonyl group. The simple method for their modifications by the reactions with electrophilic agents were elaborated and as a result of the synthetic investigation a number of N-alkyl-, N-acyl- and N-sulfonyl-4H-1,2,3-thiadiazolo[5,4-b]indoles were prepared in good yields. Preliminary biological tests for the three examples of synthesized compounds with different substituents at the nitrogen atom indole ring have shown that the biological behavior of the investigated 1,2,3-thiadiazolo[5,4-b]indoles is substantially directed by this structural fragment.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Belskaya NP,Lugovik KI,Bakulev VA,Bauer J,Kitanovic I,Holenya P,Zakhartsev M,Wölfl S

doi

10.1016/j.ejmech.2015.11.011

subject

Has Abstract

pub_date

2016-01-27 00:00:00

pages

245-257

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30348-2

journal_volume

108

pub_type

杂志文章

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