Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines
| Autor: | Dong Fang Dai, Xiao Qian Chu, Quan Zhang, Yue Chen, Jing Li, Yuan Gao, Hui Ying Li, Ye Hui Shi, Huan Gong Li, Jiang Yin, Yan Wei Dong, Zhong Sheng Tong, Chuan Ke Chong, Cui Gai Bai, Cheng Yang |
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| Rok vydání: | 2016 |
| Předmět: |
caspase-3
water soluble derivative Cell Survival Stereochemistry KG-1a Pharmaceutical Science Caspase 3 01 natural sciences Article Analytical Chemistry Sulfone sulforaphane (SFN) lcsh:QD241-441 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine lcsh:Organic chemistry Isothiocyanates Cell Line Tumor ALDH+ Drug Discovery Acids Heterocyclic Anticarcinogenic Agents Humans Tetrazole Physical and Theoretical Chemistry Cell Proliferation SUM-159 010405 organic chemistry Cell growth Organic Chemistry Sulfoxide analogues MCF-7 Aldehyde Dehydrogenase 0104 chemical sciences Gene Expression Regulation chemistry Biochemistry Chemistry (miscellaneous) Cell culture Sulfoxides 030220 oncology & carcinogenesis MCF-7 Cells Molecular Medicine Sulforaphane |
| Zdroj: | Molecules, Vol 21, Iss 4, p 514 (2016) Molecules; Volume 21; Issue 4; Pages: 514 Molecules |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules21040514 |
| Popis: | Recent studies have shown that sulforaphane (SFN) selectively inhibits the growth of ALDH⁺ breast cancer stem-like cells.Herein, a series of SFN analogues were synthesized and evaluated against breast cancer cell lines MCF-7 and SUM-159, and the leukemia stem cell-like cell line KG-1a. These SFN analogues were characterized by the replacement of the methyl group with heterocyclic moieties, and the replacement of the sulfoxide group with sulfide or sulfone. A growth inhibitory assay indicated that the tetrazole analogs 3d, 8d and 9d were significantly more potent than SFN against the three cancer cell lines. Compound 14c, the water soluble derivative of tetrazole sulfide 3d, demonstrated higher potency against KG-1a cell line than 3d. SFN, 3d and 14c significantly induced the activation of caspase-3, and reduced the ALDH⁺ subpopulation in the SUM159 cell line, while the marketed drug doxrubicin(DOX) increased the ALDH⁺ subpopulation. |
| Databáze: | OpenAIRE |
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