CHEMICO-BIOLOGICAL INTERACTION OF SELECTED TETRAHYDROPYRIMIDINES

Emilija Milović, Nenad Ž. Janković, Jelena Petronijevic, Nenad Joksimović
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Abstract

Tetrahydropyrimidines (THPMs) attracted attention as a very important class of aza heterocycles with broad pharmacological activities during the past years. In many studies have been proven that THPMs have anticancer, anti-inflammatory, antimicrobial, antioxidant, antifungal, anti-HIV activity. Bearing in mind our interest in medicinal and Biginelli chemistry, we investigated interaction with important biomacromolecules (DNA, BSA) and our earlier synthetized THPMs derivatives with proven very good cytotoxic activity.[1] Investigation of affinity of compounds A and B (Figure 1) to bind to bovine serum albumin (BSA) is based on the fact that the efficiency of drugs depends on their ability to bind for carrier protein. Binding properties were investigated by using the fluorescence emission titration of BSA with A and B. The obtained values of Ka, which are in optimum range which is considered to be 106-107M-1 indicate that both compounds have great ability to bind to BSA. In addition, Ka values for A-BSA and B-BSAshow that both compounds are suitable for drug-cell
选定四氢嘧啶的化学-生物相互作用
四氢嘧啶(tetrahydropyri嘧啶,thpm)是一类具有广泛药理活性的杂环化合物,近年来受到广泛关注。在许多研究中已经证明,thpm具有抗癌、抗炎、抗菌、抗氧化、抗真菌、抗艾滋病毒的活性。考虑到我们对药物和Biginelli化学的兴趣,我们研究了与重要生物大分子(DNA, BSA)和我们早期合成的具有良好细胞毒性活性的thpm衍生物的相互作用。[1]化合物A和B(图1)与牛血清白蛋白(BSA)结合的亲和力研究是基于药物的效率取决于它们与载体蛋白结合的能力这一事实。用荧光发射滴定法研究了A和b与牛血清白蛋白的结合特性。得到的Ka值在106 ~ 107m -1范围内,表明这两种化合物与牛血清白蛋白的结合能力都很强。此外,A-BSA和b - bsa的Ka值表明这两种化合物都适合用于药物细胞
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