Abstract
As a part of ongoing studies in developing new anticancer agents, novel 1,2-dihydropyridine
, thienopyridine
, isoquinolines
, acrylamide
, thiazolidine
, thiazoles
and thiophenes
bearing a biologically active quinoline nucleus were synthesized. The structure of newly synthesized compounds was confirmed on the basis of elemental analyses and spectral data. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. 2,3-Dihydrothiazole-5-carboxamides
,
, 4,5,6,7-tetrahydrobenzo[
]thiophene-3-carboxamide (
), 1,2-dihydroisoquinoline-7-carbonitrile (
), 5,6,7,8-tetrahydro-4
-cyclohepta[
]thiophene-3-carboxamide (
), 1,2-dihydroisoquinoline-7-carbonitrile (
),
-cyano-3-(dimethylamino)-
-(quinolin-3-yl)acrylamide (
), 1,2-dihydroisoquinoline-7-carbonitriles (
) and (
) exhibited higher activity (
values of 27–45 μmol L
) compared to doxorubicin (
47.9 μmol L
). LQ quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (
), 2-thioxo-2,3-dihydrothiazole-5-carboxamide (
) and quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (
) show activity comparable to doxorubicin, while (quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (
), 2,3-dihydrothiazole-5-carboxamide (
), thieno [3,4-
] pyridine-4(5
)-one (
), cyclopenta[
]thiophene-3-carboxamide (
) and (quinolin-3-yl)-6-stryl-1,2-dihydroisoquinoline-7-carbonitrile (
) exhibited moderate activity, lower than doxorubicin.