Synthesis and antitumor activity evaluation of 2-arylisoquinoline-1,3(2H,4H)-diones in vitro and in vivo

• DOI: 10.1007/s00044-013-0734-x
• Publication Date: 2013-08-31T13:23:23Z
• Authors: Bo-Rui Kang; Juan Wang; Huan Li; Yan Li; Qi-Bing Mei; San-Qi Zhang
• Keywords: 01 natural sciences; 0104 chemical sciences; 3. Good health

Six 2-(2-acylaminobenzothiazol-6-yl)isoquinoline-1,3(2H,4H)-diones (1a–1f) and five 2-arylisoquinoline-1,3(2H,4H)-diones (1g–1k) were synthesized by refluxing homophthalic anhydrides with 2-acylaminobenzothiazolyl-6-amine or substituted aniline in glacial acetic acid. The cytotoxic activities of 1a–1k were evaluated via MTT method against A431, A549, and PC3. Compound 1b relatively displayed a higher cytotoxic activity than the others. The antitumor effect of 1b were evaluated in established nude mice PANC-1 xenograft model. The results suggest that compound 1b could potentially inhibit tumor growth.