The Ugi4CR as effective tool to access promising anticancer isatin-based α-acetoamide carboxamide oxindole hybrids

Submitting author affiliation:
University of Évora, Évora, Portugal

Beilstein Arch. 2023, 202360.

Published 13 Dec 2023

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This preprint has not been peer-reviewed. When a peer-reviewed version is available, this information will be updated.


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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When a peer-reviewed version of this preprint is available, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:

Marques, C.; González-Bakker, A.; Padrón, J. M. Beilstein Arch. 2023, 202360. doi:10.3762/bxiv.2023.60.v1

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