Camptothecin (CPT) 是一种生物碱，作为 DNA 拓扑异构酶 I (Topo I) 抑制剂，IC50 为 679 nM。它对结直肠癌、乳腺癌、肺癌和卵巢癌表现出强效的抗肿瘤活性，并通过改变人类癌细胞中的微小 RNA (miRNA) 表达模式来调节缺氧诱导因子 1α (HIF-1α) 活性。

Irinotecan HCl Trihydrate是一种具有抗肿瘤活性的拓扑异构酶 I 抑制剂。

Topotecan is an inhibitor of topoisomerase I and the IC50 values in cancer cells are less than 6 μM.

Betulinic acid 是一种天然的五环三萜类化合物，为真核细胞拓扑异构酶 I (topoisomerase I) 的抑制剂，IC50 值为 5 μM，具有抗炎、抗疟疾、抗艾滋病和抗肿瘤等活性。

SN-38 is an active metabolite of CPT-11 that inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

Ellagic acid is a potent and cell permeable casein kinase 2 (CK2) inhibitor with Ki of 20 nM, acts as a potent antioxidant and anti-mutagenic.

β-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties and a potent inhibitor of IDO1 (IC50=0.44 μM).

(S)-10-hydroxycamptothecin is an inhibitor of DNA topoisomerase I with antitumor activity.