Synthesis and anticancer activity evaluation of some acridine derivatives
9-Amino acridine derivatives ( 1a – 1h) on condensation with 9, 10-dihydroanthracene-9, 10-α, β-succinic anhydride ( 2 ) at room temperature gave condensation products ( 3a – 3h) . Microwave-assisted condensation of 9-amino acridine derivatives ( 1a – 1d) with phthalic anhydride, cis 1,2,3,6-tetrahy...
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Veröffentlicht in: | Medicinal chemistry research 2015-05, Vol.24 (5), p.1942-1951 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 9-Amino acridine derivatives (
1a
–
1h)
on condensation with 9, 10-dihydroanthracene-9, 10-α, β-succinic anhydride (
2
) at room temperature gave condensation products (
3a
–
3h)
. Microwave-assisted condensation of 9-amino acridine derivatives (
1a
–
1d)
with phthalic anhydride,
cis
1,2,3,6-tetrahydrophthalimide, and 2,5-pyrroledione gave corresponding condensation products
4a
–
4d
,
5a
–
5d
&
6a
–
6d,
respectively, in good yields. All these compounds were screened for in vitro anticancer activity against five human cancer cell lines i.e., breast (T47D), lung (NCl H-522), colon (HCT-15), ovary (PA-1), and liver (Hep G2). Compounds
3a
(breast T47D),
3
g
(lung NCl H-522),
4a
(liver Hep G2), and
6b
(colon HCT-15) exhibited IC
50
values 5.4, 4.2, 4.5, and 2.4 µM, respectively, and hence possess good anticancer activity. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-014-1268-6 |