Abstract
The problem of designing a new drug is nowadays very important for researches representing many branches of science. This work considers the usefulness of the analytical method such as thin-layer chromatography for the lipophilicity of newly synthesized compounds, betulin derivatives, which could be potential drugs with anticancer activity. The two mobile phases were used for the purpose of experimental determination of lipophilicity for mono- and diesters investigated. The first mobile phase consists of acetate and Tris buffer, whilst the second consists of 1,4-dioxane and acetate buffer. The value of the retardation factor was recalculation into the RM value, and then RM0 values were obtained by extrapolating acetone or 1,4-dioxane concentration to zero. The chromatographic data of lipophilicity were correlated with theoretically obtained values of ALOGPS, AClogP, miLogP, ALOGP, MLOGP, XLOGP2, and XLOGP3. The particular correlation equations were obtained. The cluster analysis was also used to find similarity between the esters investigated on the basis of the experimental or theoretical value of lipophilicity obtained. The good correlation between experimentally and theoretically calculated lipophilicity gives the possibility of prediction of this value on the basis of the correlation equation. On the basis of similarity analysis was stated strong connections between the structure and the value of lipophilicity, for both experimental and theoretical values.
Highlights
Betulin and its derivatives are lately the subjects of investigation taken into consideration by a lot of researches.e betulin has the cytotoxic activity against the melanoma cells and is more cytotoxic in rapidly dividing cells which is beneficial during chemotherapy treatment [1]
E betulin has the cytotoxic activity against the melanoma cells and is more cytotoxic in rapidly dividing cells which is beneficial during chemotherapy treatment [1]
Some heterocyclic betulin derivatives show the antiparasitic activity. ey inhibit the growth of some amastigotes [4]. e other group of researchers synthesized some heterocyclic triterpenoids derived from betulin and betulinic acid [5]. e cytotoxicity to hematological tumors was observed. e antibacterial activity against five bacterial strains was investigated and confirmed for semisynthetic betulin derivatives [6]. e compounds, betulin derivatives, analyzed in this work were synthesized, and their cytotoxic properties were estimated and described [7]
Summary
Betulin and its derivatives are lately the subjects of investigation taken into consideration by a lot of researches.e betulin has the cytotoxic activity against the melanoma cells and is more cytotoxic in rapidly dividing cells which is beneficial during chemotherapy treatment [1]. E antibacterial activity against five bacterial strains was investigated and confirmed for semisynthetic betulin derivatives [6]. E compounds, betulin derivatives, analyzed in this work were synthesized, and their cytotoxic properties were estimated and described [7]. E other derivatives of betulin were synthesized, and their anticancer activity was analyzed by the same group of scientists [9, 10]. E popular and often-used method is the shakeflask method [11] It is based on extraction in the octanolwater system [11]. E shake-flask method causes problems in the case of polar or highly lipophilic substance. It requires the high purity of the substance analyzed and the solute [13]
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