Two mononuclear Pt(II) compounds, [Pt(BQL1)Cl]Cl (BQL1-Pt) and [Pt(BQL2)Cl]Cl (BQL2-Pt), with [5-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-pentyl]-bis-pyridin-2-ylmethyl-amine (BQL1) and [9-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-nonyl]-bis-pyridin-2-ylmethyl-amine (BQL2), were prepared as new chemotypes for potential antitumor agents. In this study, the effects of cryptolepine derivatives in BQL1-Pt, 2,2′-dipicolylamine Pt(II) complex, and BQL2-Pt on cellular Pt(II) accumulation, cytotoxicity, and in vitro and in vivo antitumor activities against T-24 cancer cells and normal HL-7702 cells were evaluated. BQL1-Pt and BQL2-Pt displayed cytotoxic activities in the micromolar range (1.3 ± 0.1 and 0.2 ± 0.2 μM, respectively) on T-24 cancer cells; however, they did not exhibit any toxicity against HL-7702 cells. They triggered T-24 cell apoptosis through a mitochondrial dysfunction pathway. BQL1-Pt and BQL2-Pt prepared from the neutral BQL1 and BQL2 ligands with cryptolepine derivatives showed better antitumor activities than 2,2′-dipicolylamine. Furthermore, BQL2-Pt effectively inhibited the growth of bladder T-24 tumor in vivo. BQL2-Pt could be a potential therapeutic candidate for cancers.

两种单核Pt（II）化合物[Pt（BQL1）Cl] Cl（BQL1-Pt）和[Pt（BQL2）Cl] Cl（BQL2-Pt），具有[5-（苯并[4,5]]呋喃[3] ，2-b] quinolin-11-yloxy）-pentyl]-双吡啶-2-基甲基胺（BQL1）和[9-（benzo [4,5] furo [3,2-b] quinolin-11-作为潜在的抗肿瘤药物的新化学型，制备了（氧基）-壬基]-双吡啶-2-基甲基胺（BQL2）。在这项研究中，BQL1-Pt，2,2'-二甲基吡啶胺Pt（II）配合物和BQL2-Pt中的隐血平衍生物对细胞Pt（II）积累，细胞毒性以及针对T的体内和体外抗肿瘤活性的影响评价了-24个癌细胞和正常的HL-7702细胞。BQL1-铂和BQL2 -铂显示细胞毒活性在微摩尔范围（1.3±0.1和0.2±0.2μM，分别地）在T-24癌细胞; 然而，它们对HL-7702细胞没有任何毒性。他们通过线粒体功能障碍途径触发了T-24细胞凋亡。由中性BQL1和BQL2配体与隐血藤碱衍生物制备的BQL1-Pt和BQL2-Pt显示出比2,2'-二甲基吡啶胺更好的抗肿瘤活性。此外，BQL2-Pt在体内有效抑制膀胱T-24肿瘤的生长。BQL2-Pt可能是潜在的癌症治疗药物。