Li-Juan Yang

Preparation and characterization of inclusion complexes of naringenin with β-cyclodextrin or its derivative.

The inclusion complexation behavior, characterization and binding ability of naringenin with β-cyclodextrin and its derivatives were investigated in both solution and the solid state by means of XRD, DSC, SEM, (1)H and 2D NMR and UV-vis spectroscopy. The results showed that the water solubility and thermal stability of naringenin were obviously increased in the inclusion complex with cyclodextrins. This satisfactory water solubility and high thermal stability of the naringenin/CD complexes will be potentially useful for their application as herbal medicines or healthcare products.

Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole.

A series of novel hybrid compounds between 2-phenylbenzofuran and imidazole have been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that substitution of the imidazolyl-3-position with a naphthylacyl or bromophenacyl group, were vital for modulating cytotoxic activity. In particular, hybrid compound 15 was found to be the most potent compound against 4 strains human tumor cell lines and more active than cisplatin (DDP), and exhibited cytotoxic activity selectively against liver carcinoma (SMMC-7721).

Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds

A series of novel hybrid compounds of 2-phenyl-3-alkylbenzofuran and imidazole or triazole were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 2-ethyl-imidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or naphthylacyl group, were vital for modulating inhibitory activity. In particular, hybrid compound 31 was found to be the most potent derivative with IC₅₀ values of 0.08-0.55 μM against five strains human tumor cell lines and was found to be more selective against breast carcinoma (MCF-7) and colon carcinoma (SW480) (IC₅₀ values 40.8-fold and 40.1-fold lower than cisplatin (DDP)).

Design, synthesis and cytotoxic activities of novel hybrid compounds between dihydrobenzofuran and imidazole

A series of novel hybrid compounds between dihydrobenzofuran and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that substitution of the imidazolyl-1-position with an electron-donating dihydrobenzofuran, and the imidazolyl-3-position with a naphthylacyl or electron-rich phenacyl group, were vital for modulating cytotoxic activity.

Novel 3-substituted fluorine imidazolium/triazolium salt derivatives: synthesis and antitumor activity

A series of novel (+/-)-3-substituted fluorene-imidazolium/triazolium salt derivatives has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of 2-methyl-benzimidazole or 5,6-dimethyl-benzimidazole rings and substitution of the imidazolyl/triazolyl3/4-position with a naphthylacyl or 4-methoxyphenacyl group were important for modulating cytotoxic activity. Compounds 37 and 42 were found to be the most potent derivatives with IC50 values of 0.51-2.51 mu M and exhibited cytotoxic activities selectively against myeloid leukaemia (HL-60), liver carcinoma (SMMC-7721) and lung carcinoma (A549). Compound 37 can remarkably induce the G2/M phase cell cycle arrest and apoptosis in SMMC-7721 cells. Additionally, compound 30 exhibited selective cytotoxicity to some extent between cancer cells (A549) and normal cells (BEAS-2B).

Novel Tricyclic Indeno[5,6-b]furan-imidazole Hybrid Compounds: Design, Synthesis and Antitumor Activity

A series of novel hybrid compounds between tricyclic indeno[5,6-b] furan and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl group were vital for modulating cytotoxic activity. In particular, hybrid compound 26 was found to be the most potent compound against 5 strains human tumor cell lines and more active than cisplatin (DDP), while compound 18 was more selective towards breast carcinoma (MCF-7) and colon carcinoma (SW480) with IC50 value 3.4-fold and 4.3-fold more sensitive to DDP.