3,3-Disubstituted oxindole derivatives bearing a nitrogen atom at the C-3 position have been synthesized starting from 3-alkyl oxindole through a metal free pathway. These derivatives have been tested in five human tumor cell lines (PC3, MCF7, SW620, MiaPaca2 and A375) and on primary cells (PBMCs) from healthy donors providing compound 6d showing a strong anticancer effect in all cancer lines on the low micromolar range.

Novel 3,3-disubstituted oxindole derivatives. Synthesis and evaluation of the anti-proliferative activity / M. Christodoulou, F. Nicoletti, K. Mangano, M.A. Chiacchio, G. Facchetti, I. Rimoldi, E.M. Beccalli, S. Giofrè. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 30:2(2020 Jan 15). [10.1016/j.bmcl.2019.126845]

Novel 3,3-disubstituted oxindole derivatives. Synthesis and evaluation of the anti-proliferative activity

M. Christodoulou
Primo
;
G. Facchetti;I. Rimoldi;E.M. Beccalli
Penultimo
;
S. Giofrè
Ultimo
2020

Abstract

3,3-Disubstituted oxindole derivatives bearing a nitrogen atom at the C-3 position have been synthesized starting from 3-alkyl oxindole through a metal free pathway. These derivatives have been tested in five human tumor cell lines (PC3, MCF7, SW620, MiaPaca2 and A375) and on primary cells (PBMCs) from healthy donors providing compound 6d showing a strong anticancer effect in all cancer lines on the low micromolar range.
3,3-Disubstituted oxindole; Anti-proliferative activity; Human cancer cell lines; Iminophosphorane; Isocyanate;
Settore CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
   PIANO DI SOSTEGNO ALLA RICERCA 2015-2017 - LINEA 2 "DOTAZIONE ANNUALE PER ATTIVITA' ISTITUZIONALE"
   UNIVERSITA' DEGLI STUDI DI MILANO
15-gen-2020
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/700732
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