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Novel substituted (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-diones and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones as potent radio-sensitizing agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2009-11-22 , DOI: 10.1016/j.bmcl.2009.11.082 Y Thirupathi Reddy 1 , Konjeti R Sekhar , Nidhish Sasi , P Narsimha Reddy , Michael L Freeman , Peter A Crooks
中文翻译:
新型取代的(Z)-5-((N-苄基-1H-吲哚-3-基)亚甲基)咪唑烷-2,4-二酮和5-((N-苄基-1H-吲哚-3-基)亚甲基)嘧啶-2,4,6(1H,3H,5H)-三酮作为有效的放射增敏剂
更新日期:2009-11-22
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2009-11-22 , DOI: 10.1016/j.bmcl.2009.11.082 Y Thirupathi Reddy 1 , Konjeti R Sekhar , Nidhish Sasi , P Narsimha Reddy , Michael L Freeman , Peter A Crooks
Affiliation
A series of (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-dione (9a–9m) and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-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.
中文翻译:
新型取代的(Z)-5-((N-苄基-1H-吲哚-3-基)亚甲基)咪唑烷-2,4-二酮和5-((N-苄基-1H-吲哚-3-基)亚甲基)嘧啶-2,4,6(1H,3H,5H)-三酮作为有效的放射增敏剂
一系列 ( Z )-5-(( N -benzyl-1 H -吲哚-3-基)亚甲基)咪唑烷-2,4-二酮 ( 9a – 9m ) 和 5-(( N -benzyl-1 H -吲哚-3-基)亚甲基)嘧啶-2,4,6(1 H ,3 H ,5 H )-三酮 ( 10a – 10i ) 衍生物在吲哚和N-苄基部分均包含多种芳香族取代基被合成。评估了这些类似物对 HT-29 细胞系的放射增敏活性。三种类似物10a 、 10b和10c被确定为最有效的放射增敏剂。