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Benzoquinones are class of natural quinones found chiefly in higher plants, fungi, bacteria and animal kingdom. They are involved in important biological functions such as bioenergetic transport, oxidative phosphorylation and electron transport processes. In recent years it has become increasingly clear that some of them possess potent antioxidant, anti-inflammatory and anticancer activities. There is clearly a common thread running through these activities and there have been a large number of studies carried out to unravel the mechanisms of these activities. In the present review we have provided a brief account of these studies especially covering these aspects. Although antioxidant potentials of these compounds constitute the basis of their biological activities its nature and scope is dictated by many microscopic biological environments. One of the important advantages offered by these compounds is the ease with which they can be synthesized and chemically manipulated. This can easily provide impetus for further research in developing some potentially useful drug molecules.

Purpose Pancreatic cancer (PC) is one of the deadliest of all tumors. Previously, we were the first to show that Thymoquinone (TQ) derived from black seed (Nigella sativa) oil has anti-tumor activity against PC. However, the concentration of TQ required was considered to be high to show this efficacy. Therefore, novel analogs of TQ with lower IC50 are highly desirable. Methods We have synthesized a series of 27 new analogs of TQ by modifications at the carbonyl sites or the benzenoid sites using single pot synthesis and tested their biological activity in PC cells. Results Among these compounds, TQ-2G, TQ-4A1 and TQ-5A1 (patent pending) were found to be more potent than TQ in terms of inhibition of cell growth, induction of apoptosis and modulation of transcription factor-NF-κB. We also found that our novel analogs were able to sensitize gemcitabine and oxaliplatin-induced apoptosis in MiaPaCa-2 (gemcitabine resistant) PC cells, which was associated with down-regulation of Bcl-2, Bcl-xL, survivin, XIAP, COX-2 and the associated Prostaglandin E2. Conclusion From our results, we conclude that three of our novel TQ analogs warrant further investigation against PC, especially in combination with conventional chemotherapeutic agents.

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Recent developments on structural studies of bis-phenols and related compounds are systematically discussed. The effects of substituents on bis-phenols to control the size and shape of cavities in assemblies of bis-phenols and the weak interactions in anion-assisted assemblies of bis-phenols are narrated to illustrate pseudo-polymorphism. The possible impact of the occurrence of a high Z′ value in different polymorphs of bis-phenol and related compounds is presented.

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