No abstract

No abstract

Agents which can recognize and bind specific sequences of DNA offer selective therapy through the modulation of specific transcription factors or genes. Recently, there has been renewed interest in the field of anticancer minor groove binders. This may be attributed to the fact that many compounds of this class have demonstrated significant antitumor activity against a wide variety of cancers in recent clinical trials. This review will discuss the recent efforts to overcome the drawbacks of existing minor groove binding anticancer agents through rational drug design based on scaffolds with known antitumor activity.

No abstract

In the reaction of 3,4‐dihydroquinoline (IX) an aromatization is observed which does not take place using isoquinolines.

No abstract

A diverse array of polyheterocyclic annulated 1,2,3‐triazolo‐fused‐tetrahydro‐β‐carboline derivatives have been synthesized via an intramolecular azide‐alkyne cycloaddition (1,3‐dipolar) reaction. Among the hexaheterocyclic series 5 a–r, the compound 5 b (14,15‐dimethoxy‐6,7,12,12b‐tetrahydro‐4H‐benzo[5′,6′][1,2,3]triazolo[5′′,1′′:3′,4′][1,4]diazepino[1′,7′:1,2]pyrido[3,4‐b]indole) displayed significant cytotoxicity against the MCF‐7 cell line with an IC50 value of 6.45 ± 0.37 μM; whereas, among the pentaheterocyclic series 14 a–l, the derivative 14 b ((6R,12aS)‐6‐(3,4‐dimethoxyphenyl)‐7,12,12a,13‐tetrahydro‐4H,6H‐[1,2,3]triazolo[1′′,5′′:4′,5′]pyrazino[1′,2′:1,6]pyrido[3,4‐b]indole) has shown potent cytotoxicity with an IC50 value of 4.01 ± 0.39 μM on the B16F10 cell line. Treatment of MCF‐7 and B16F10 cells with 5 b and 14 b respectively resulted in cell cycle arrest, inhibition of cell migration and colony formation as well as induction of apoptosis. DNA binding affinity estimation by viscometry experiment and molecular modeling revealed their efficient minor groove binding.

A stable and isolable Cu(i) complex has been identified for the direct oxidative synthesis of α-ketoamides in water.