Several quinazoline derivatives have been found to possess a broad spectrum of biological activities. Previously our research group has synthesized and studied the anti-proliferative effects of N-Decyl-N-(2-Methyl-4-Quinazolinyl) Amine (DMQA). The current study evaluated the cytotoxic and apoptotic properties of DMQA in THP-1 cells. The cytotoxic potential of DMQA was assessed using MTT assay on a panel of cancer cell lines which include HeLa, Mia PaCa-2, A 375, B16-F10, A 549,A 431, U937, THP-1, HL-60 and peripheral blood mononuclear cells (PBMC's). Preliminary data revealed that the highest cytotoxic activity was against THP-1 leukemia cell line (IC₅₀₌0.66 μg/ml). The apoptotic properties of DMQA on THP-1 cells were characterized by change in nuclear morphology, DNA fragmentation, reduction of pro-caspases-3, 9, Bax/Bcl-2 levels, cleavage of poly (ADP-ribose) polymerase and cytosolic release of cytochrome c. Further investigation revealed a sub-G1 peak, phosphatidyl serine exposure and loss of mitochondrial membrane potential (MMP) in THP-1 cells. The role of caspases was crucial and was demonstrated by the inhibitors Z-VAD-FMK and Z-DEVD-FMK. Moreover DMQA was markedly less effective in inhibiting the growth of normal cells (PBMC's, IC_{50 =}62.17 μg/ml). Based on the results we suggest that DMQA induced apoptosis via intrinsic pathway and could be a promising anticancer agent.

已经发现几种喹唑啉衍生物具有广泛的生物活性。以前，我们的研究小组已经合成并研究了N-癸基-N-（2-甲基-4-喹唑啉基）胺（DMQA）的抗增殖作用。目前的研究评估了DMQA在THP-1细胞中的细胞毒性和凋亡特性。DMQA的细胞毒性潜力是在一系列癌细胞系（包括HeLa，Mia PaCa-2，A 375，B16-F10，A 549，A 431，U937，THP-1，HL-60和外周血）上使用MTT分析评估的血液单核细胞（PBMC）。初步数据显示，最高的细胞毒性活性是针对THP-1白血病细胞系（IC _{50 =}0.66μg/ ml）。DMQA在THP-1细胞上的凋亡特性的特征在于核形态变化，DNA片段化，前胱天蛋白酶3、9，Bax / Bcl-2水平降低，多聚（ADP-核糖）聚合酶裂解和胞质释放细胞色素c。进一步的研究表明，THP-1细胞中存在一个亚G1峰，磷脂酰丝氨酸暴露和线粒体膜电位（MMP）的损失。半胱天冬酶的作用至关重要，并由抑制剂Z-VAD-FMK和Z-DEVD-FMK证实。此外，DMQA在抑制正常细胞生长方面效果显着（PBMC's，IC _{50 =} 62.17μg/ ml）。根据结果​​，我们认为DMQA通过内在途径诱导细胞凋亡，并且可能是一种有前途的抗癌药。