The anti-cancer activity of the benzo[h]quinolines was evaluated on cultured human skin cancer (G361), lung cancer (H460), breast cancer (MCF7) and colon cancer (HCT116) cell lines. The inhibitory effect of these compounds on the cell growth was determined by the MTT assay. The compounds 3e, 3f, 3h and 3j showed potential cytotoxicity against these human cancer cell lines. Effect of active compounds on DNA oxidation and expression of apoptosis related gene was studied. We also developed a quantitative method to measure the activity of cyclin-dependent kinases-2 (CDK2) by western blotting in the presence of active compound. In addition, molecular docking revealed that benzo[h]quinolines can correctly dock into the hydrophobic pocket of the targets receptor protein aromatase and CDK2, while their bioavailability/drug-likeness was predicted to be acceptable but requires future optimization. These findings reveal that benzo[h]quinolines act as anti-cancer agents by inducing oxidative stress-mediated DNA damage.
5 August 2009 in Journal of the American Chemical Society
Thieno[3,2-c]pyran was synthesized as a fluorescent turn-on chemosensor for the selective recognition of Zn2+ ions with a low detection limit (0.67 μM), and it also exhibited AIE properties.
Alkynes are a very important class of compounds and used as precursors for the assembly of a variety of carbocycles and heterocycles. Alkynes are classified into two classes: terminal alkynes and internal alkynes. Terminal alkynes were used as one of the precursors for the synthesis of internal alkynes. Besides, various elimination reactions were conducted to obtain alkynes. Various applications of alkynes are known but no compiled review is reported so far regarding their synthesis. Therefore, we have compiled the literature available for the synthesis of various functionalized alkynes from non-alkyne sources in this review. We have not discussed the synthesis of internal alkynes from terminal alkynes. Based on the available literature, the synthesis of alkynes can be classified into three major types of reactions: (a) synthesis of alkynes through α,β-elimination, (b) synthesis of alkynes through carbene rearrangement and (c) synthesis of alkynes via miscellaneous approaches. In this review, we have focused on the different methods available for these transformations including their scope, limitations and recent developments. We have also discussed the mechanism involved during the reaction.