Beilstein Arch. 2023, 202360. https://doi.org/10.3762/bxiv.2023.60.v1
Published 13 Dec 2023
Considering early-stage drug discovery programmes, the Ugi four component reaction is a valuable, flexible, and pivotal tool, facilitating the creation of two new amide bonds in a one-pot fashion to effectively yield the desired a-aminoacyl amides. Here, we highlight the reputation of this reaction approach to access number and scaffold diversity of a library of isatin-based a-acetoamide carboxamide oxindole hybrids, promising anticancer agents, in a mild and fast sustainable reaction process. The library was tested against six human solid tumor cell lines, among them, non-small cell lung carcinoma, cervical adenocarcinoma, breast cancer and colon adenocarcinoma. The most potent compounds 8d, 8h and 8k showed GI50 values in the range of 1-10 uM.
Keywords: Ugi4CR; cancer; oxindole; GI50; isatin
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Marques, C.; González-Bakker, A.; Padrón, J. M. Beilstein Arch. 2023, 202360. doi:10.3762/bxiv.2023.60.v1
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