Venkataramanan Natarajan Sathiyamoorthy, Suvitha Ambigapathy, Sahara Ryoji
Department of Chemistry, School of Engineering, Dayanada Sagar University, Bangalore 562 112, India.
Department of Chemistry, SKP Engineering College, Tiruvannamalai 606 601, India.
Molecules. 2025 Jun 25;30(13):2732. doi: 10.3390/molecules30132732.
The adsorption of the drug gemcitabine on nucleobases was investigated using a dispersion-corrected density functional theory (DFT) study. The planar structure of complexes is more stable than those with stacked and buckle-angled configurations. The complexes were found to possess at least two intermolecular hydrogen bonds. The binding energy and interaction energy are both negative, with the highest values observed for the gemcitabine-guanine and the lowest in the gemcitabine-thymine complex. The complex formation was found to be an enthalpy-driven process. Pyrimidine nucleobases have a lower enthalpy of formation than purine nucleobases. The computed HOMA and NICS values on the gemcitabine-nucleobase complexes show a substantial increase compared to the pristine nucleobases. An MESP analysis of the complexes shows a directional interaction and electron density shift between the gemcitabine and the nucleobases. A QTAIM analysis indicates that the intermolecular hydrogen bonds have a partial covalent character. The computed bond energy demonstrates that intermolecular NH⋅⋅⋅N bonds are more potent than other bonds. An energy decomposition analysis using the DLPNO-CCSD(T) method indicates that the complexes exhibit a substantial electrostatic attraction, and dispersion contributes the least towards the system stability. The intermolecular bonds are stronger than the intramolecular bonds in the drug-nucleobase complexes. The strength of intramolecular bonds is determined by the deformation of the gemcitabine ring during the complex formation.
采用色散校正密度泛函理论(DFT)研究了吉西他滨药物在核碱基上的吸附情况。配合物的平面结构比具有堆积和扣角构型的结构更稳定。发现这些配合物至少具有两个分子间氢键。结合能和相互作用能均为负值,在吉西他滨 - 鸟嘌呤配合物中观察到最高值,而在吉西他滨 - 胸腺嘧啶配合物中最低。发现配合物的形成是一个焓驱动的过程。嘧啶核碱基的生成焓比嘌呤核碱基低。与原始核碱基相比,计算得到的吉西他滨 - 核碱基配合物的HOMA和NICS值有显著增加。配合物的MESP分析显示了吉西他滨与核碱基之间的定向相互作用和电子密度转移。QTAIM分析表明分子间氢键具有部分共价特征。计算得到的键能表明分子间NH⋅⋅⋅N键比其他键更强。使用DLPNO - CCSD(T)方法进行的能量分解分析表明,配合物表现出显著的静电吸引力,且色散对体系稳定性的贡献最小。在药物 - 核碱基配合物中,分子间键比分子内键更强。分子内键的强度由配合物形成过程中吉西他滨环的变形决定。