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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:30

Article

Christodoulou, Michael S.¹  Nicoletti, Ferdinando²  Mangano, Katia²  Chiacchio, Maria Assunta³  Facchetti, Giorgio¹  Rimoldi, Isabella¹  Beccalli, Egle M.¹  Giofre, Sabrina¹ 

[1] Univ Milan, Sez Chim Gen & Organ A Marchesini, DISFARM, Via Venezian 21, I-20133 Milan, Italy

[2] Univ Catania, BIOMETEC, Via Santa Sofia 97, I-95123 Catania, Italy

[3] Univ Catania, Dipartimento Sci Farmaco, Viale Andrea Doria 6, I-95125 Catania, Italy

关键词: 3,3-Disubstituted oxindole;    Isocyanate;    Iminophosphorane;    Anti-proliferative activity;    Human cancer cell lines;   

DOI  :  10.1016/j.bmcl.2019.126845

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

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