The ability of a number of nitrogen-containing compounds that simultaneously carry the adamantane and monoterpene moieties to inhibit Tdp1, an important enzyme of the DNA repair system, is studied. Inhibition of this enzyme has the potential to overcome chemotherapeutic resistance of some tumor types. Compound (+)-3c synthesized from 1-aminoadamantane and (+)-myrtenal, and compound 4a produced from 2-aminoadamantane and citronellal were found to be most potent as they inhibited Tdp1 with IC₅₀ values of 6 and 3.5 µM, respectively. These compounds proved to have low cytotoxicity in colon HCT-116 and lung A-549 human tumor cell lines (CC₅₀ > 50 µM). It was demonstrated that compound 4a at 10 µM enhanced cytotoxicity of topotecan, a topoisomerase 1 poison in clinical use, against HCT-116 more than fivefold and to a lesser extent of 1.5 increase in potency for A-549.

研究了同时带有金刚烷和单萜部分的多种含氮化合物抑制Tdp1（DNA修复系统的重要酶）的能力。抑制这种酶具有克服某些肿瘤类型的化学治疗抗性的潜力。发现由1-氨基金刚烷和（+）-myrtenal合成的化合物（+）- 3c以及由2-氨基金刚烷和香茅醛产生的化合物4a最有效，因为它们抑制Tdp1的IC ₅₀值分别为6和3.5 µM。这些化合物在结肠HCT-116和肺A-549人肿瘤细胞系中被证明具有低细胞毒性（CC ₅₀  > 50 µM）。已证明化合物4a 当浓度为10 µM时，临床上使用的拓扑异构酶1毒物拓扑替康对HCT-116的细胞毒性提高了5倍以上，对A-549的效价提高幅度较小，为1.5。