Full
Outline
The rate constant of the bioorthogonal cleavage reaction is a critical parameter for its in vivo translation and application. Building upon the bioorthogonal decaging chemistry of silylborane and N-oxide, this study conducted structural optimization toward silylborane to obtain derivatives with higher second-order rate constants. The structure-reactivity relationships studies revealed that introducing electron-withdrawing groups onto the phenyl ring of the silylbenzyl moiety significantly enhanced the cleavage reaction rate. Furthermore, several silylboranes were successfully identified with fast reaction kinetics (k2 > 102 L·mol-1·s-1). A representative derivative 2b (k2 = 239 L·mol-1·s-1) was able to efficiently and specifically activate the N-oxide based fluorescent probe and prodrug of tamoxifen at the cellular level. In summary, this work provides an efficient cleavage reaction tool for the design of bioorthogonal prodrugs for in vivo applications.
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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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