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Title 

A novel stereo-selective sulfonylurea, -[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4- phenyl-imidazolidin-2-one, has antitumor efficacy in in vitro and in vivo tumor models

Authors 

Chang Woo LeeDong Ho HongSang Bae HanS H JungHyoung-Chin KimR L FineSang-Han LeeHwan Mook Kim

Publisher 

Elsevier

Issue Date 

2002

Citation 

Biochemical Pharmacology, vol. 64, no. 3, pp. 473-480

Keywords 

antitumor agentsin vitro and in vivo tumor modelsstereo-selectivesulfonylureas1 [1 (4 aminobenzoyl) 2,3 dihydro 1h indol 6 sulfonyl] 4 phenylimidazolidin 2 onedw 2143dw 2282sulfonylurea derivativeunclassified druganimal cell

Abstract 

The antitumor activities of novel 1-[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4-phenyl- imidazolidin-2-ones were studied to determine the potential of these compounds as antitumor candidates. The agents studied were: DW2143 (1-[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4-phenyl- imidazolidin-2-one), a racemic mixture, and DW2282 [(4S)-1-[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4-phenyl- imidazolidin-2-one], an S-isomer. DW2143 and DW2282 suppressed the in vitro growth of tumor cells at lower concentrations than doxorubicin, but tumor specificity was not observed between the compounds. These compounds when administered orally were not active in syngeneic models of murine Colon 26 adenocarcinoma and L1210 leukemia. However, DW2143 suppressed the growth of SW620 (human colon cancer) and NCI-H23 (human lung cancer) cells in nude mice, inhibiting tumor growth by 87 and 67%, respectively. DW2282 was a more potent inhibitor of SW620 tumor cell growth in nude mice and was also lower in toxicity than DW2143. Moreover, DW2282 did not produce a series of toxic symptoms caused by the aniline metabolites of sulfonylureas, including hypoglycemia. These results suggest that DW2282, an S-isomer, could be a novel antitumor candidate with higher specificity and lower toxicity than other orally active sulfonylureas.

ISSN 

0006-2952

Link 

http://dx.doi.org/10.1016/S0006-2952(02)01105-X

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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