Wu Chun-Zhen, Lai Long, Hu Xiao, Lei Rong-Rong, Yang Yi-Fang
a State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry , Shanghai , 200040 , China.
J Asian Nat Prod Res. 2013 Sep;15(9):993-1002. doi: 10.1080/10286020.2013.823950. Epub 2013 Aug 14.
Tetrandrine possesses antitumor activity, however, only a few studies on its structure modification were reported. To improve the antitumor activity of tetrandrine, 20 new tetrandrine derivatives were designed and synthesized by Sonogashira and Suzuki reactions. Their antitumor activities were evaluated against three tumor cell lines including A549, HepG2, and BGC-823 by methyl thiazolyl tetrazolium assay with taxol as a positive control. The results showed that compounds 2c and 2g were highly potent against BGC-823 cell line, and compounds 1i and 1k showed particular activity against HepG2 cells. These results demonstrated that compounds 1i, 1k, 2c, and 2g were promising leads for further investigation.
粉防己碱具有抗肿瘤活性，然而，关于其结构修饰的研究报道较少。为了提高粉防己碱的抗肿瘤活性，通过Sonogashira反应和Suzuki反应设计并合成了20种新的粉防己碱衍生物。以紫杉醇为阳性对照，采用甲基噻唑基四唑𬭩盐法对其对包括A549、HepG2和BGC-823在内的三种肿瘤细胞系的抗肿瘤活性进行了评价。结果表明，化合物2c和2g对BGC-823细胞系具有高效活性，化合物1i和1k对HepG2细胞表现出特殊活性。这些结果表明，化合物1i、1k、2c和2g是值得进一步研究的有前景的先导化合物。
