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ATP-citrate lyase (ACLY), serving as a critical energy metabolism bridge in tumor cells, is closely implicated in the development of various malignancies. Inhibition or knockout of ACLY has been reported to effectively suppress tumor cell proliferation and induce apoptosis. In this work, we have designed and synthesized 18 dehydrocurvularin cinnamy ACLY inhibitors. Through biological evaluation and molecular dynamics simulations, we systematically explored the structure-activity relationships (SAR) of these derivatives. Compound 4e exhibited potent anti-proliferative activity against MDA-MB-231 and PANC-1 cells with a IC50 value of 0.4 and 1.1 μmol·L-1, providing crucial insights for structural modification and SAR studies of this class of macrolide derivatives.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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