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

• Carolina S. Marques,
• Aday González-Bakker and
• José M. Padrón

Beilstein J. Org. Chem. 2024, 20, 1213–1220, doi:10.3762/bjoc.20.104

• 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 μM. Keywords: cancer; GI50; isatin; oxindole; Ugi4CR; Introduction Meticulous attention has been given by

• processes, a second family of α-acetamide carboxamide oxindole derivatives 5 was obtained using the previously optimized Ugi4CR approach [16] (Scheme 2 and Figure 2). Taking into account the preliminary SAR studies reported for the first family of Ugi-derived isatin-peptoids, the second family was obtained

• conditions (120 ºC, 30 minutes) (Scheme 3). Resourcefulness of the Ugi4CR and preliminary SAR studies [16] lead us to synthesize a third library of oxindole derivatives, using trifluoroacetic acid (TFA), under mild reaction conditions, to afford the corresponding α-acetamide carboxamide isatin hybrids 8 from