Abstract

A series of dibenzodiazepine 2-position derivatives, bearing N-methylpiperazine at the C-11 position, were prepared by using a concise approach. Their inhibitory activities of tumor cell proliferation in vitro were tested in five cell lines, including breast cancer cell BCAP37, gastric cancer cell SGC7901, liver cancer cell HepG2, cervical cancer cell HeLa and acute promyelocytic leukemia cell HL-60. Several compounds showed efficient tumor activity with IC₅₀ values down to 0.30 μM. These compounds are expected to be a new class of potential anticancer lead compounds.

Graphic abstract

中文翻译：

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二苯二氮卓类衍生物抗肿瘤活性的合成与评价

摘要

通过使用简洁的方法制备了一系列在 C-11 位带有N-甲基哌嗪的二苯并二氮杂2-位衍生物。在五种细胞系中测试了它们的体外肿瘤细胞增殖抑制活性，包括乳腺癌细胞BCAP37、胃癌细胞SGC7901、肝癌细胞HepG2、宫颈癌细胞HeLa和急性早幼粒细胞白血病细胞HL-60。几种化合物显示出有效的肿瘤活性，IC ₅₀值低至 0.30 μM。这些化合物有望成为一类新的潜在抗癌先导化合物。

图形摘要