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Concise synthesis of carbazole-1,4-quinones and evaluation of their antiproliferative activity against HCT-116 and HL-60 cells.

Abstract：

:We report a convenient synthesis of carbazole-1,4-quinone alkaloid koeniginequinones A and B using a tandem ring-closing metathesis with the dehydrogenation reaction sequence under an O2 atmosphere as an important step. Using this method, carbazole-1,4-quinones substituted at the 5-, 6-, 7-, and/or 8-positions have been synthesized. Moreover, 24 compounds, including koeniginequinones A and B, have been evaluated for their antiproliferative activity against HCT-116 and HL-60 cells, and the 6-nitro analog exhibited the most potent activity against both tumor cell types.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Nishiyama T,Hatae N,Yoshimura T,Takaki S,Abe T,Ishikura M,Hibino S,Choshi T

doi

10.1016/j.ejmech.2016.05.065

subject

Has Abstract

pub_date

2016-10-04 00:00:00

pages

561-577

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30473-1

journal_volume

121

pub_type

杂志文章

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