卟啉
化学
G-四倍体
组合化学
体外
虚拟筛选
MTT法
端粒
DNA
立体化学
生物化学
药效团
作者
Rajendra Bhadane,D B Meshram,Ritu Gilhotra
出处
期刊:PubMed
日期:2017-11-01
卷期号:12 (2): 103-111
摘要
G-quadruplex structures formed in telomeres and proto-oncogene represent a potentially useful target for anticancer drugs. Stabilization of this arrangement may inhibit the further action of different enzymes involved in cancer cell immortalization. In present work structure based drug design and synthesis was carried out on series of meso-substituted porphyrin analogues. The interaction of porphyrin derivatives with G-quadruplex DNA has been explored by virtual screening procedure. Some of the potential binding agents were then synthesized and evaluated in-vitro by MTT and PCR stop assay. The study indicates that these compounds had strong G-Quadruplex binding affinity with very good inhibitory activity in MCF-7 and A549 cell lines.
科研通智能强力驱动
Strongly Powered by AbleSci AI