Aplysinopsin analogs: Synthesis and anti-proliferative activity of substituted ( Z)-5-( N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones
A series of substituted ( Z)-5-( N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione ( 3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating m...
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Published in | Bioorganic & medicinal chemistry Vol. 18; no. 10; pp. 3570 - 3574 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
England
Elsevier Ltd
15.05.2010
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Subjects | |
Online Access | Get full text |
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Summary: | A series of substituted (
Z)-5-(
N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (
3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and
N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods. These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs,
3f and
3j had IC
50 values of 4.4 and 5.2
μM, respectively, compared to 5-fluorouracil (IC
50
=
15.2
μM) against MCF-7 cells.
A series of substituted (
Z)-5-(
N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (
3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and
N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs,
3f and
3j had IC
50 values of 4.4 and 5.2
μM, respectively, compared to 5-fluorouracil (IC
50
=
15.2
μM) against MCF-7 cells. |
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ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2010.03.054 |