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Title 

Structure-activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity

Authors 

S SubramanianN S KimP ThanigaimalaiV K SharmaK C LeeJ S KangHwan Mook KimS H Jung

Publisher 

Elsevier

Issue Date 

2011

Citation 

European Journal of Medicinal Chemistry, vol. 46, no. 8, pp. 3258-3264

Keywords 

Anticancer activityAntimitotic agentArylsulfonylimidazolidinone

Abstract 

To define the SAR, a series of novel N-arylsulfonylimidazolidinone derivatives were evaluated for their in vitro anticancer activity against five human tumor cell lines, including A549, COLO205, KATO III, K562, SK-OV-3 and murine leukemia (P288D1) cell line. Among them, N-(2-chloroacetyl)-6-(2-oxo-4- phenylimidazolidin-1-ylsulfonyl)-3,4-dihydroquinoline-1(2H)-carboxamide (4m) and N-cyclohexyl-6-(2-oxo-4-phenylimidazolidin-1-ylsulfonyl)-3,4-dihydroquinoline- 1(2H)-carboxamide (4n) exhibited comparable in vitro anticancer activity to doxorubicin against A549, KATO III and K562 cell lines and gave superior xenographic results against NCI-H23 and SW620 cancer cell lines. Regarding the structure-activity relationship, two critical points were discovered; the steric congestion at 4-position of N-arylsulfonylimidazolidinone scaffold abolishes the activity and the bulkiness or hydrophobicity of acyl groups at 3,4-dihydroquinoline of 4, especially with carbamoyl moiety, enormously enhances the activity.

ISSN 

0223-5234

Link 

http://dx.doi.org/10.1016/j.ejmech.2011.04.042

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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