tetraindoles, a second generation of the compounds with changes in the core phenyl ring was synthesized to improve anticancer properties. 17 new compounds with different rigidity, planarity, symmetry and degree of conjugation of their core structures to 5-hydroxyindole units were synthesized. All the compounds were fully characterized and tested against breast cancer cell line (MDA-MB-231). The results
在最初成功地优化一系列新的四
吲哚的基础上,合成了第二代在核心苯环中具有变化的化合物,以提高抗癌性能。合成了17种新化合物,这些化合物具有不同的刚性,平面度,对称性和核心结构与
5-羟基吲哚单元的共轭程度。所有化合物均经过充分表征,并针对乳腺癌
细胞系(
MDA-MB-231)进行了测试。结果表明,核心结构是活性所必需的,它应该是芳香的,刚性的,平面的,对称的和共轭的,以实现最佳活性。化合物29对多种肿瘤来源的
细胞系具有强大的抗癌活性,包括Mahlavu(肝细胞),SK-HEP-1(肝),HCT116(结肠),MIA PaCa-2(胰腺),H441(肺乳头), A549(肺),经过一系列连续优化后,产生了H460(非小细胞肺癌)和CL1-5(肺癌),IC50值在0.19至3.50μM之间。已发现在患有异种移植的MIA PaCa-2人胰腺癌的非肥胖型糖尿病重度联合免疫缺陷(NOD / SCID)小鼠