185098-72-0Relevant academic research and scientific papers
Structure-activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity
Subramanian, Santhosh,Kim, Nam-Soo,Thanigaimalai, Pillaiyar,Sharma, Vinay K.,Lee, Ki-Cheul,Kang, Jong Seong,Kim, Hwan-Mook,Jung, Sang-Hun
scheme or table, p. 3258 - 3264 (2011/08/03)
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.
Synthesis and evaluation of cytotoxic activity of novel arylsulfonylimidazolidinones
Jung, Sang-Hun,Song, Jae-Shin,Lee, Hui-Soon,Choi, Sang-Un,Lee, Chong-Ock
, p. 2553 - 2558 (2007/10/03)
Synthesis of novel arylsulfonylimidazolidinones 3 and 4 containing sulfonylurea pharmacophore and evaluation of their in vitro cytotoxicity against human cell lines were investigated. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolidinones have been found to be the potential anticancer agent.
