intercalation

BMH-21 是一种小分子 DNA 嵌入剂，可结合核糖体 DNA 并抑制 RNA 聚合酶 I (Pol I) 转录，具有抗癌活性。

UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物，具有强大的抗肿瘤活性，能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性，但由于限制剂量的骨髓毒性，目前尚未进入三期临床试验。相比之下，UNBS3157的最大耐受剂量比Amonafide高出3-4倍，并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外，在活体内模型中，包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中，UNBS3157显示出优于Amonafide的效果。

MitoNeoD is a novel mitochondria-targeted O2(⋅−) probe that can be used in vivo. It prevents DNA intercalation. MitoNeoD incorporates a carbon-deuterium bond, and enhances O2(⋅−) selectivity.

YO-Pro 1 是一种由苯并恶唑和喹啉环通过连接体连接而成的菁染料，在水中几乎没有荧光，但其荧光在插入双链DNA后大大增强，成为DNA浓度测定的基础，Ex Em (结合DNA) = 491 509 nm。YO-Pro 1 可用于鉴定凋亡细胞。

Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.

Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.

Cyclopentenylcytosine（CPC）是一种核苷类似物，通过抑制CTP合成酶来降低白血病细胞中的胞苷三磷酸（CTP）和脱氧胞苷三磷酸（dCTP）水平。此外，Cyclopentenylcytosine 促进 1-β-D-阿拉伯核糖甘露苷胞苷(araC)的磷酸化并增加其插入DNA的活性。Cyclopentenylcytosine 以浓度（50-300 nM）和时间依赖（8-16小时）的方式诱导人T淋巴细胞系MOLT-3的凋亡和坏死。Cyclopentenylcytosine与araC联合使用可以增强对凋亡和坏死的诱导作用及其在T淋巴母细胞中的细胞毒性。