Cytotoxicities of the quinolizidine alkaloid (–)-cytisine and 19 of its derivatives with substituents in the 3-, 9-, and 11-positions were assessed against A431 (epidermal carcinoma), A375 (melanoma), and HCT 116 (colorectal carcinoma) tumor cell lines using the MTT assay (etoposide reference drug). Practically all synthesized compounds at a concentration of 30 μM possessed slight ability to inhibit metabolic activity of these cell lines except benzylcytisine 4, methylcytisines 18 and 19, which contained a phenylurea fragment in the 9- or 11-position of the 2-pyridone core, and 11-chloro adamantylthiocarboxamide 16. Thiocarboxamide 16 reduced A431 cell survival up to 56.06% under the experimental conditions; derivatives 4, 18, and 19, of HCT 116 cell line by 57.52, 58.84, and 56.34%, respectively.

中文翻译：

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几种 Cytisine 衍生物的合成及其对 A431、A375 和 HCT 116 肿瘤细胞系的细胞毒性

针对 A431（表皮癌）、A375（黑色素瘤）和 HCT 116（结直肠癌）评估了喹诺利西啶生物碱 (-)-胞嘧啶及其 19 种在 3-、9- 和 11-位具有取代基的衍生物的细胞毒性使用 MTT 测定法（依托泊苷参考药物）的肿瘤细胞系。除了苄基胞嘧啶 4、甲基胞嘧啶 18 和 19 外，几乎所有浓度为 30 μM 的合成化合物都具有轻微的抑制这些细胞系代谢活性的能力，它们在 2-吡啶酮核心的 9 位或 11 位含有苯基脲片段，和11-氯金刚烷基硫代甲酰胺16。硫代甲酰胺16在实验条件下使A431细胞存活率降低达56.06%；HCT 116 细胞系的衍生物 4、18 和 19 分别增加了 57.52、58.84 和 56.34%。