癌症常常与突变性微管蛋白和微管活性的异常增加相关，后者对于细胞的迁移、入侵和转移至关重要。一系列新型的脂肪酸共轭茉莉酮被设计为微管聚合抑制剂和抗癌药物候选。这些共轭物被设计来利用两类自然成分的有益物理化学特性、易于合成和抑制微管活性。新脂化茉莉酮从4-氨基乙酮经N-酰化和不同芳香醛缩合合成。所有新化合物在低浓度下展现出对乳腺癌和肺癌细胞株（MCF-7和A549）的微管聚合抑制和抗增殖活性。流式细胞术证实新化合物具有明显的凋亡作用，并通过3-[4,5-二甲基硫唑-2-基]-2,5-二苯基四氮唑溴化物测定表明具有细胞毒性。癸酸共轭物比较长的类似物更为强效，最活跃的比参比微管抑制剂combretastatin-A4和抗癌药物doxorubicin更为强效。没有一个新合成的化合物在100 μM以下引起Wi-38正常细胞系的明显细胞毒性或红细胞溶血。由于它们脂质的性质，描述的新结合物不太可能影响正常细胞或干扰细胞膜。进行了定量结构活性关系分析，以确定315种描述符对于新结合物的物理化学特性对其微管抑制活性的影响。得到的模型揭示了所调查化合物的微管抑制活性与它们的偶极矩和反应程度之间的强相关性。

Cancer is often associated with an aberrant increase in tubulin and microtubule activity required for cell migration, invasion, and metastasis. A new series of fatty acid conjugated chalcones have been designed as tubulin polymerization inhibitors and anticancer candidates. These conjugates were designed to harness the beneficial physicochemical properties, ease of synthesis, and tubulin inhibitory activity of two classes of natural components. New lipidated chalcones were synthesized from 4-aminoacetophenone via N-acylation followed by condensation with different aromatic aldehydes. All new compounds showed strong inhibition of tubulin polymerization and antiproliferative activity against breast and lung cancer cell lines (MCF-7 and A549) at low or sub-micromolar concentrations. A significant apoptotic effect was shown using a flow cytometry assay that corresponded to cytotoxicity against cancer cell lines, as indicated by a 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay. Decanoic acid conjugates were more potent than longer lipid analogues, with the most active being more potent than the reference tubulin inhibitor, combretastatin-A4 and the anticancer drug, doxorubicin. None of the newly synthesized compounds caused any detectable cytotoxicity against the normal cell line (Wi-38) or hemolysis of red blood cells below 100 μM. It is unlikely that the new conjugates described would affect normal cells or interrupt with cell membranes due to their lipidic nature. A quantitative structure-activity relationship analysis was performed to determine the influence of 315 descriptors of the physicochemical properties of the new conjugates on their tubulin inhibitory activity. The obtained model revealed a strong correlation between the tubulin inhibitory activity of the investigated compounds and their dipole moment and degree of reactivity.