Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
Eur J Med Chem. 2012 Sep;55:455-61. doi: 10.1016/j.ejmech.2012.06.057. Epub 2012 Jul 7.
1H-1,2,3-triazole tethered isatin conjugates have been synthesized and evaluated for cytotoxicity on four human cancer cell lines. The results revealed 5a, 5c, 5e and 5n proved to be twice as potent as 5-fluorouracil on THP-1 cell line with 5a and 5c being most active exhibiting IC(50) values of <1 against all cell lines except Caco-2. Activity profiles showed dependence on the substituents on isatin rings with a preference for hydrogen while a strong electron withdrawing fluoro as well as nitro substituents on either ring decreased the anticancer activity.
1H-1,2,3-三氮唑键合的色酮缀合物已被合成，并对四种人癌细胞系的细胞毒性进行了评估。结果表明，5a、5c、5e 和 5n 在 THP-1 细胞系上的效力是 5-氟尿嘧啶的两倍，其中 5a 和 5c 的活性最高，对除 Caco-2 以外的所有细胞系的 IC50 值均<1。活性谱显示对色酮环上取代基的依赖性，对氢有偏好，而在任一环上具有强吸电子氟和硝基取代基则降低了抗癌活性。
