Structural Modification Of 6-substituted Carbazole Ring And Its Antitumor Activity In Vitro

The carbazole and pyridine derivatives have a wide range of pharmacological activities,such as:antibacterial,antiviral,anti-inflammatory,antitumor,etc.As an active site,carbazole and pyridine compounds have a non-negligible role in enhancing molecular activity.This topic is based on the research work of single-target antitumor drugs in recent years.With carbazole as lead compound,pyridine derivatives are molecular fragments,using the principle of active group splicing,A total of 14 carbazole urea and carbazole amine derivatives were synthesized.All the synthesized compounds were confirmed by 1HNMR,13CNMR and MS.Anti-tumor activity tested using MTT assay,The test cells were HepG2,A549,Hela,AsPC-1,respectively;The test concentration is 10?M,the results show:The activities of the target compounds A2,A3,B5,B7,B8,B9,B10 and B11 are more prominent,the inhibition rate of A549 and Hela was 100%at 10 ?M.The inhibition rate of AsPC-1 by B5,B8,and B10 was 100%.The inhibition rate of AsPC-1 by B5,B8,and B10 was 100%.The inhibition rates of HepG2 by A2,B5,B7,B8,B9,and B10 also reached 100%.After consulting the literature,it was confirmed that none of the synthesized compounds was reported in the literature.This verified that carbazole carbamide and carbazole amine compounds conjugated by carbazole and pyridine derivatives have excellent activity in anti-tumor and wide development space.