Novel substituted ( Z)-5-(( N-benzyl-1 H-indol-3-yl)methylene)imidazolidine-2,4-diones and 5-(( N-benzyl-1 H-indol-3-yl)methylene)pyrimidine-2,4,6(1 H,3 H,5 H)-triones as potent radio-sensitizing agents
A series of ( Z)-5-(( N-benzyl-1 H-indol-3-yl)methylene)imidazolidine-2,4-dione ( 9a– 9m) and 5-(( N-benzyl-1 H-indol-3-yl)methylene)-pyrimidine-2,4,6(1 H,3 H,5 H)-trione ( 10a–10i) derivatives that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized....
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Published in | Bioorganic & medicinal chemistry letters Vol. 20; no. 2; pp. 600 - 602 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
Amsterdam
Elsevier Ltd
15.01.2010
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A series of (
Z)-5-((
N-benzyl-1
H-indol-3-yl)methylene)imidazolidine-2,4-dione (
9a–
9m) and 5-((
N-benzyl-1
H-indol-3-yl)methylene)-pyrimidine-2,4,6(1
H,3
H,5
H)-trione (
10a–10i) derivatives that incorporate a variety of substituents in both the indole and
N-benzyl moieties have been synthesized. These analogs were evaluated for their radiosensitization activity against the HT-29 cell line. Three analogs,
10a,
10b, and
10c, were identified as the most potent radio-sensitizing agents.
A series of (
Z)-5-((
N-benzyl-1
H-indol-3-yl)methylene)imidazolidine-2,4-dione (
9a–
9m) and 5-((
N-benzyl-1
H-indol-3-yl)methylene)pyrimidine-2,4,6(1
H,3
H,5
H)-trione (
10a–
10i) derivatives that incorporate a variety of aromatic substituents in both the indole and
N-benzyl moieties have been synthesized. These analogs were evaluated for their radiosensitization activity against the HT-29 cell line. Three analogs,
10a,
10b, and
10c were identified as the most potent radiosensitizing agents. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 These authors equally contributed to this Letter. |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.11.082 |