Two structurally novel series of histone deacetylase inhibitors (HDACIs) involving two potential surface recognition moieties; 3′,4′-dihydro-2′H-spiro[imidazolidine-4,1′-naphthalene]-2,5-dione (in series I) and 1-(3-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamide (in series II) were designed, synthesized, and evaluated for their anti-proliferative activities, HDAC inhibitory activities, and their binding modes to HDAC protein. Compounds 5f and 10e showed comparable HDAC inhibitory activity to SAHA.

Series II have been also demonstrated as potential HDAC-tubulin dual inhibitors, promoted with structural similarities between (1-(3-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamide) nucleus, of series II, and Combretastatin A4.

The tubulin inhibitory activities of series II members, together with their docking into colchicine binding site of β-tubulin were performed. Compound 9a showed remarkable cytotoxicity. Hybrid 10e behaved as potent HDAC-tubulin dual inhibitor. It showed better tubulin inhibition than CA4 as well as its effectiveness against HDAC.

两个结构上新颖的系列组蛋白脱乙酰基酶抑制剂（HDACI），涉及两个潜在的表面识别部分；3'，4'-二氢-2' ħ -螺[咪唑烷4,1'萘〕-2,5-二酮（串联I）和1-（3-甲氧基苯基）-5-（3,4-，设计，合成并合成了5-三甲氧基苯基）-1H-1,2,4-三唑-3-羧酰胺（系列II），它们具有抗增殖活性，HDAC抑制活性以及它们与HDAC蛋白的结合方式。化合物5f和10e显示出与SAHA相当的HDAC抑制活性。

II系列也已被证明是潜在的HDAC-微管蛋白双重抑制剂，其在（1-（3-甲氧基苯基）-5-（3,4,5-三甲氧基苯基）-1H-1,2,4-三唑-系列II（3-羧酰胺）核和Combretastatin A4。

进行了系列II成员的微管蛋白抑制活性，以及​​它们对接至β-微管蛋白的秋水仙碱结合位点。化合物9a显示出显着的细胞毒性。Hybrid 10e表现为有效的HDAC-微管蛋白双重抑制剂。它显示出比CA4更好的微管蛋白抑制作用，以及对HDAC的有效性。