- 英文名称
- (R)-1-((1H-Imidazol-5-yl)methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile
- 分子式
- C25H23N5O2S2
- 分子量
- 489.61
- 中文别名
- BMS-214662; 1-((1H-咪唑-4-基)甲基)-3-苄基-4-(噻吩-2-基磺酰基)-2,3,4,5-四氢-1H-苯并[e][1,4]二氮杂卓-7-甲腈; 化合物T10567; (3R)-2,3,4,5-四氢-1-(1H-咪唑-5-基甲基)-3-(苯基甲基)-4-(2-噻吩基磺酰基)-1H-1,4-苯并二氮杂环庚烷-7-氰基; 化合物BMS-214662; BMS-214662; BMV; (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile; 3-BENZYL-1-(1H-IMIDAZOL-4-YLMETHYL)-4-(THIEN-2-YLSULFONYL)-2,3,4,5-TETRAHYDRO-1H-1,4-BENZODIAZEPINE-7-CARBONITRILE; 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine; (R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile; (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile; (4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile
- 用途
- 作为farnesyl transferase抑制剂，具有抗肿瘤活性；靶点IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)；体外研究显示对多种肿瘤细胞系有抑制作用，体内研究显示可增加肿瘤细胞凋亡，提高AI值，对HCT-116和EJ-1肿瘤细胞有细胞毒性。
