Ju-Lian Li's research while affiliated with Sichuan University and other places

A series of novel indolylquinones have been synthesized by treating halogeno-quinone with 2-substituated indole derivatives in the presence of kalium carbonate and TEBA in acetonitrile at room temperature. These compounds were evaluated for their antiproliferative activity against human MDA-MB-231 and MCF-7 breast cancer cell lines. All the tested compounds showed potent mircomolar cytotoxicity activity in both breast cancer cell lines. 3d (IC(50) value=2.29 μg/mL for MCF-7 cells) and 3g (IC(50) value=3.99 μg/mL for MDA-MB-231 cells) displayed the most potent antiproliferative activity of the series. Also, in vitro anticancer activity of the compounds further showed that bis-indolylquinones were more active than mono-indolylquinones. Fluorescence microscopy analysis indicated that compound 3d and 3g inhibited breast cancer cells proliferation by triggering apoptotic cell death.

A convenient and effective method for the synthesis of vinylphosphonates (III) (16 examples), which exhibit antitumor activities, is given.

Ruthenium(II)-porphyrin (0.5 mol%) catalyzed N-imidations of aromatic nitrogen heterocycles with phenyl(tosylimino)iodinane under mild conditions were achieved in good yields (<94%). The effects of substituent, catalyst, temperature, and solvent on the reaction have been investigated. It was found that the catalyst significantly affected the yield and selectivity of imidation reaction for aromatic nitrogen heterocycles at 30 degrees C.

A rapid method for the selective cleavage of aryl methyl ether in the lithium chloride-N,N-dimethylformamide (LiCl-DMF) system under microwave irradiation has been developed. Effects of substituent, metal salt and solvent on the activity and selectivity in the cleavage reaction have been investigated. It is found that microwave significantly improves the reaction yield and the selectivity of demethylation for electron deficient aromatic methyl ethers. The catalytic mechanism of demethylation by LiCl salt is proposed.

To evaluate apoptosis induced by rehenium-188-labeled diethylenetriamine pentaacetic acid-glucosamine (188Re-DTPA-DG) in MCF-7 breast carcinoma cells and A549 pulmonary carcinoma cells. Through the use of flow cytometry (FCM) with CBA software to detect apoptosis, cells of both the MCF-7 and A549 cell lines were divided into groups exposed to 188Re-DTPA-DG, 188Re-perrhenate (188ReO4-), and saline, respectively. The first two groups were further divided into subgroups on the basis of their exposure to radioactivity at 37, 55.5, or 74 kBq/mL, with the saline-exposed group divided into three corresponding subgroups. Each subgroup was introduced into 5 replicate wells of a culture plate, and the morphology of the cells in each well was determined by flow cytometry at 6-hour intervals for 18 hours. In order to determine the affinity of 188Re-DTPA-DG for tumor tissue, the biodistribution of the radiolabeled agent was assessed in breast tumor-bearing nude mice. Change in morphology of the cell nucleus was more evident in the 188Re-DTPA-DG-treated than in the 188ReO4--treated group, and no change in nuclear morphology was seen in the saline-exposed group. The study data suggested that there was a greater ratio of apoptotic to nonapoptotic cells among the 188Re-DTPA-DG-treated than among the 188ReO4--treated or saline-exposed cells (p<0.01), and a greater change in cell-nuclear morphology in the 188Re-DTPA-DG-treated than in the 188ReO4--treated cells. Furthermore, 188Re-DTPA-DG had a more significant apoptosis-inducing effect on both MCF-7 and A549 cells than did 188ReO4-. The biodistribution study in tumor-bearing nude mice showed that the concentration of 188Re-DTPA-DG in tumor tissue was much higher than in normal tissue, that 188Re-DTPA-DG was rapidly cleared from the blood, and that the main route of its clearance was via the kidneys. 188Re-DTPA-DG has a significant apoptotic effect on carcinoma cells. 188Re-DTPA-DG is an effective radiopharmaceutical for intratumoral radiation therapy.

Melatonin was prepared from phthalimide by N- and C-alkylation, cyclization, hydrolytic, decarboxylation, and acetylation. The four-pot reactions were carried out on microwave irradiation in good yield with short time.