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Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions.

Abstract：

:Interaction of 2-iodoaniline or 5-fluoro-2-iodoaniline with a range of arylsulfonyl chlorides affords sulfonamides that undergo Sonogashira couplings under thermal or microwave conditions with the alkyne 4-ethynyl-4-hydroxycyclohexa-2,5-dien-1-one followed by cyclization to 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclo-hexa-2,5-dien-1-ones. This method allows for incorporation of a range of substituents into the arylsulfonyl moiety, and compounds showed selective in vitro inhibition of cancer cell lines of colon and renal origin, a feature of compounds bearing the quinol pharmacophore.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

McCarroll AJ,Bradshaw TD,Westwell AD,Matthews CS,Stevens MF

doi

10.1021/jm061163m

subject

Has Abstract

pub_date

2007-04-05 00:00:00

pages

1707-10

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

50

pub_type

杂志文章

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