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色酮基噻唑烷的合成及其对人癌细胞系的细胞毒性。

Synthesis of chromonylthiazolidines and their cytotoxicity to human cancer cell lines.

作者信息

Anh Hoang Le Tuan, Cuc Nguyen Thi, Tai Bui Huu, Yen Pham Hai, Nhiem Nguyen Xuan, Thao Do Thi, Nam Nguyen Hoai, Van Minh Chau, Van Kiem Phan, Kim Young Ho

机构信息

Institute of Marine Biochemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam.

Institute of Biotechnology, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam.

出版信息

Molecules. 2015 Jan 12;20(1):1151-60. doi: 10.3390/molecules20011151.

Abstract

Nine new chromonylthiazolidine derivatives were successfully semi-synthesized from paeonol. All of the compounds, including starting materials, the intermediate compound and products, were evaluated for their cytotoxic effects toward eight human cancer cell lines. The synthesized chromonylthiazolidines displayed weak cytotoxic effects against the tested cancer cell lines, but selective cytotoxic effects were observed. Compounds 3a and 3b showed the most selective cytotoxic effects against human epidermoid carcinoma (IC50 44.1 ± 3.6 μg/mL) and breast cancer (IC50 32.8 ± 1.4 μg/mL) cell lines, respectively. The results suggest that chromoylthiazolidines are potential low-cost, and selective anticancer agents.

摘要

从丹皮酚成功地半合成了九种新的色酮基噻唑烷衍生物。对所有化合物,包括起始原料、中间化合物和产物,进行了它们对八种人类癌细胞系的细胞毒性作用评估。合成的色酮基噻唑烷对测试的癌细胞系显示出较弱的细胞毒性作用,但观察到了选择性细胞毒性作用。化合物3a和3b分别对人表皮样癌(IC50 44.1±3.6μg/mL)和乳腺癌(IC50 32.8±1.4μg/mL)细胞系表现出最具选择性的细胞毒性作用。结果表明,色酮基噻唑烷是潜在的低成本、选择性抗癌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1fab/6272249/7f68ab8e75e8/molecules-20-01151-g001.jpg

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