Park Sujin, Kim Eun Hye, Kim Jinwoo, Kim Seong Hwan, Kim Ikyon
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea.
Center for Drug Discovery Technology, Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
Eur J Med Chem. 2018 Jan 20;144:435-443. doi: 10.1016/j.ejmech.2017.12.056. Epub 2017 Dec 19.
A new chemical space was explored based on an indolizine-chalcone hybrid, which was readily accessible by base-mediated aldol condensation of indolizine bearing a 7-acetyl group with various (hetero)aromatic aldehydes. Their anticancer effect was evaluated, revealing that indolizine-chalcone hybrids with 3,5-dimethoxyphenyl group (4h) or the halogen at the meta position (4j and 4l) could have the potential to induce the caspase-dependent apoptosis of human lymphoma cells.
基于中氮茚-查尔酮杂化物探索了一个新的化学空间，该杂化物可通过带有7-乙酰基的中氮茚与各种（杂）芳族醛进行碱介导的羟醛缩合反应轻松获得。评估了它们的抗癌效果，结果表明具有3,5-二甲氧基苯基（4h）或间位卤素（4j和4l）的中氮茚-查尔酮杂化物可能具有诱导人淋巴瘤细胞半胱天冬酶依赖性凋亡的潜力。
