Effect of side chain location in (2-aminoethyl)-aminomethyl-2-phenylquinolines as antitumor agents.
Bioorg Med Chem Lett
; 8(10): 1243-8, 1998 May 19.
Article
in En
| MEDLINE
| ID: mdl-9871743
ABSTRACT
Three new derivatives of 2-phenylquinoline having an (2-aminoethyl)aminomethyl group in 7-, 6-, or 4'- (para position of 2-phenyl ring) positions of aromatic system have been prepared. The antitumor activity of these compounds together with 8- or 4- substituted isomers against the HeLa cell is in the order of 8- > 7- > 4- approximately 6- approximately 4'- substituted ones, which is almost in good agreement with that of DNA-binding ability evaluated by means of DNA-titration of UV-VIS spectra, DNA melting experiment, and ethidium displacement assay. Two representative compounds (8- and 4- isomers) are confirmed to have an ability to intercalate into double stranded DNA by topoisomerase I superhelix unwinding assay.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinolines
/
DNA
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
1998
Document type:
Article
Affiliation country: