Anti-tumor compound and the medical use thereof

US10512627B2 · kind B2 · utility

Assignee

• Tianjin Medical University Cancer Institute and Hospital · CN

Inventors

• Ning Zhang · Tianjin, CN
• Yinsong Wang · Tianjin, CN
• Ping Zhou · Plainsboro, US
• Hua Guo · Nanhu, CN
• Yi Luo · Shanghai, CN
• Xishan Hao · Tianjin, CN
• Hua Geng · Tianjin, CN

Key dates

• Filing date: Sep 2, 2015
• Grant date: Dec 24, 2019
• Expiry date: Sep 22, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C231/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention disclose a compound of formula (I), wherein, R1 is selected from —H or C1-C6 hydrocarbon group, —NH2, —OH, —O(CH2)nCH3 (n=0, 1 or 2), —N(CH3)2, or —CH2N(CH3)2, R2 is selected from an amino acid or an hydroxy acid or —OH (R1, R2 are not —CH3 and —OH at the same time), wherein X, Y are —H, —CH3, —CH2OH, —CH(OH)CH3, —CH2SH, —CH(CH3)2, —CH2CH(CH3)2, —CH(CH3)CH2CH3, —CH2CH2SCH3, —CH2COOH, —CH2CONH2, —CH2CH2COOH, —CH2CH2CH2CH2NH2, or —CH2CH2CONH2, R3-R5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.