The process of drug discovery includes individual synthesis and characterization of drug candidates, followed by a biological screening, which is separated from synthesis in space and time. This approach suffers from low throughput and associated high costs, which in turn lead to inefficiency in the field of drug discovery. Here, we present a miniaturized platform combining combinatorial solid-phase synthesis with high-throughput cell screenings. The method is based on the formation of nanoporous poly(2-hydroxyethyl methacrylate-co-ethylene dimethacrylate) layers patterned with hydrophilic spots separated from each other by superhydrophobic liquid-impermeable barriers. The porous polymer inside the hydrophilic spots is used as a support to conduct solid-phase synthesis. The hydrophilic spots can be then filled with droplets containing either reagents for synthesis or live cells. Upon irradiation with UV light, products of solid-phase synthesis are released from the porous polymer because of the photo-cleavable linkers used and diffuse into separate droplets. The light-induced release of the products allows the control of the release spatially, temporally, and quantitatively. To demonstrate the versatility and usability of the platform for various cell lines, we have successfully implemented peptide synthesis to create an exemplary chemical library and demonstrated high cell viability after the UV-triggered small-molecule release.

药物发现的过程包括候选药物的单独合成和表征，然后进行生物学筛选，该生物学筛选在空间和时间上与合成分离。该方法遭受低通量和相关的高成本的困扰，这继而导致药物发现领域的低效率。在这里，我们提出了一个小型的平台，结合了组合固相合成和高通量细胞筛选。该方法基于纳米多孔聚（甲基丙烯酸2-羟乙酯-co-二甲基丙烯酸乙二酯）层，其上形成有亲水斑点，并通过超疏水性液体不可渗透的屏障彼此隔开。亲水点内部的多孔聚合物用作进行固相合成的载体。然后可以用包含用于合成的试剂或活细胞的液滴填充亲水性斑点。在用紫外线照射时，由于所用的光可裂解的连接基，固相合成的产物从多孔聚合物中释放出来并扩散成单独的液滴。产品的光诱导释放允许在空间，时间和数量上控制释放。为了展示该平台对于各种细胞系的多功能性和可用性，