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3 results on '"Prostate cancer cell line"'

1. Synthesis of Flavone Derivatives via N-Amination and Evaluation of Their Anticancer Activities

Author

Chao Chen, Jun-Rong Song, Wei-Dong Pan, Jun Luo, Zhang Ni, Su Yang, Ke Li, and Jin Yang

Subjects
Cell Survival, Stereochemistry, antiproliferation, flavone, Pharmaceutical Science, Antineoplastic Agents, Chemistry Techniques, Synthetic, 010402 general chemistry, 01 natural sciences, Article, Analytical Chemistry, lcsh:QD241-441, Structure-Activity Relationship, chemistry.chemical_compound, lcsh:Organic chemistry, Cell Line, Tumor, Drug Discovery, medicine, Humans, Physical and Theoretical Chemistry, IC50, Amination, Cell Proliferation, chemistry.chemical_classification, Cisplatin, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Chemistry, Flavone derivatives, Organic Chemistry, Flavones, Anticancer drug, 0104 chemical sciences, Amino acid, anticancer activity, Prostate cancer cell line, Chemistry (miscellaneous), Apigenin, Molecular Medicine, amino acid, medicine.drug
Abstract

Seventeen new flavone derivatives substituted at the 4&prime, OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure&ndash, activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.

Published
2019
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2. A Useful Synthesis of 2-Acylamino-1,3,4-oxadiazoles from Acylthiosemicarbazides Using Potassium Iodate and the Discovery of New Antibacterial Compounds

Author

Song Wu, Li Tianlei, Jishun Li, Wenxuan Zhang, and Gang Wen

Subjects
medicine.drug_class, Potassium Compounds, Antibiotics, Iodates, Pharmaceutical Science, Bacillus subtilis, Chemistry Techniques, Synthetic, Microbial Sensitivity Tests, 010402 general chemistry, medicine.disease_cause, 01 natural sciences, Article, Analytical Chemistry, lcsh:QD241-441, chemistry.chemical_compound, Minimum inhibitory concentration, lcsh:Organic chemistry, Drug Discovery, medicine, Humans, Physical and Theoretical Chemistry, IC50, Potassium iodate, Oxadiazoles, heterocycles, biology, Bacteria, 010405 organic chemistry, Chemistry, Organic Chemistry, biology.organism_classification, 0104 chemical sciences, Anti-Bacterial Agents, Semicarbazides, antibacterial, Prostate cancer cell line, 2-acylamino-1,3,4-oxadiazoles, Chemistry (miscellaneous), Staphylococcus aureus, Molecular Medicine, synthetic method, Nuclear chemistry
Abstract

A useful method for the synthesis of 2-acylamino-1,3,4-oxadiazoles was developed. By using potassium iodate as an oxidant in water at 60 &deg, C, a wide range of 2-acylamino-1,3,4-oxadiazoles were afforded in moderate to excellent yields within two hours. This method could provide a facile shortcut to generate a series of 2-acylamino-1,3,4-oxadiazoles in medicinal chemistry. Interestingly, some highly potent antibiotic compounds were found through this synthetic method, and some of them displayed a significant improvement in activity compared with the corresponding 1,4-diacylthiosemicarbazides. Compound 2n was the most active against Staphylococcus aureus with MIC (minimum inhibitory concentration) of 1.56 mg/mL, and compounds 2m and 2q were the most active against Bacillus subtilis with MIC of 0.78 mg/mL. The preliminary cytotoxic activities of the most potent compounds 2m, 2n, and 2q against the androgen-independent (PC-3) prostate cancer cell line were more than 30 &mu, M (IC50 &gt, 30 &mu, M).

Published
2019
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3. Antioxidant and Anticancer Activities of Essential Oil from Gannan Navel Orange Peel

Author

Chen Hongli, Chao Yang, Balian Zhong, Xuzhong Luo, Hui Chen, and Chun Jiong

Subjects
0301 basic medicine, Antioxidant, Cell Survival, medicine.medical_treatment, Cell Culture Techniques, Pharmaceutical Science, Orange (colour), anticancer, Antioxidants, Article, essential oil, Analytical Chemistry, law.invention, lcsh:QD241-441, 03 medical and health sciences, chemistry.chemical_compound, lcsh:Organic chemistry, law, Cell Line, Tumor, Drug Discovery, Botany, Cyclohexenes, medicine, Oils, Volatile, Humans, Plant Oils, MTT assay, Food science, Physical and Theoretical Chemistry, Essential oil, Limonene, Human lung cancer, Plant Extracts, Terpenes, Organic Chemistry, Gannan navel orange, Antineoplastic Agents, Phytogenic, 030104 developmental biology, chemistry, Prostate cancer cell line, Chemistry (miscellaneous), Fruit, Molecular Medicine, Navel orange, GC-MS, Citrus sinensis
Abstract

China is one of the leading producers of citrus in the world. Gannan in Jiangxi Province is the top navel orange producing area in China. In the present study, an essential oil was prepared by cold pressing of Gannan navel orange peel followed by molecular distillation. Its chemical composition was analyzed by GC-MS. Twenty four constituents were identified, representing 97.9% of the total oil. The predominant constituent was limonene (74.6%). The anticancer activities of this orange essential oil, as well as some of its major constituents, were investigated by MTT assay. This essential oil showed a positive effect on the inhibition of the proliferation of a human lung cancer cell line A549 and prostate cancer cell line 22RV-1. Some of the oil constituents displayed high anticancer potential and deserve further study.

Published
2017

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