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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Fatty acyl amide derivatives of doxorubicin: synthesis and in vitro anticancer activities.
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Fatty acyl amide derivatives of doxorubicin: synthesis and in vitro anticancer activities.

机译：阿霉素的脂肪酰基酰胺衍生物：合成和体外抗癌活性。

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摘要

Doxorubicin is extensively used in anticancer therapy. Doxorubicin is highly hydrophilic, has short half-life, and its use is associated with severe side effects at high doses. Fatty acyl amide derivatives of doxorubicin were synthesized with the expectation to improve the lipophilicity and anticancer activity of the drug. The lipophilicity was enhanced with the increase in chain length of fatty acyl moiety. Conjugation of 4'-amino group with fatty acids through an amide bond reduced the anticancer activity in leukemia, breast, ovarian, and colon cancer cell lines, suggesting that the presence of free amino group is required for anticancer activity of doxorubicin. Dodecanoyl-doxorubicin derivative was consistently the most effective among the synthesized derivatives and inhibited the proliferation of colon (HT-29) and ovarian (SK-OV-3) cancer cells by 64% and 58%, respectively, at a concentration of 1 muM after 96 h incubation.
机译：阿霉素被广泛用于抗癌治疗。阿霉素是高度亲水的，半衰期短，其使用与高剂量时的严重副作用有关。合成了阿霉素的脂肪酰基酰胺衍生物，以期改善该药物的亲脂性和抗癌活性。亲脂性随脂肪酰基部分链长的增加而增强。通过酰胺键将4'-氨基与脂肪酸结合，降低了白血病，乳腺癌，卵巢癌和结肠癌细胞系的抗癌活性，这表明阿霉素的抗癌活性需要游离氨基的存在。在合成的衍生物中，十二烷酰-阿霉素衍生物一直是最有效的，浓度为1μM时，结肠癌（HT-29）和卵巢癌细胞（SK-OV-3）的增殖分别分别抑制64％和58％孵育96小时后。

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