Gold(I)-Catalyzed Synthesis of 4H-Benzo[d][1,3]oxazines and Biological Evaluation of Activity in Breast Cancer Cells.

The first gold(I)-catalyzed cycloisomerization procedure applied to the synthesis of substituted 4H-benzo[d][1,3]oxazines has been developed starting from N-(2-alkynyl)aryl benzamides. The chemoselective oxygen cyclization via the 6-exo-dig pathway yielded the observed heterocycles in modest to good chemical yields under very mild reaction conditions. The obtained oxazines were assayed on the breast cancer (BC)-derived cell lines MCF-7 and HCC1954 with differential biological activity. The newly synthesized 4H-benzo[d][1,3]oxazine compounds showed several degrees of cell proliferation inhibition with a remarkable effect for those compounds having a substituted aryl at C-2 of the molecules. The 4H-benzo[d][1,3]oxazines showed an IC50 ranking from 3.1 to 95 µM in MCF-7 and HCC1954 cells. These compounds represent potential drug candidates for BC treatment. However, additional assays are needed to elucidate their complete effect over the cellular and molecular hallmarks of cancer.

Outcome of tobacco cessation in workplace and clinic settings: A comparative study.

AIMS AND OBJECTIVES: Several biological, social, and cultural factors contribute to the poor outcome of tobacco cessation interventions. Inability to engage large number of participants is one of the major identifiable factors. The objective of this study was to compare the outcome of tobacco cessation interventions in the clinical and workplace settings. MATERIALS AND METHODS: In the present study, we recruited 100 participants in tobacco cessation clinic (TCC) group and workplace group (50 participants in each). Both the groups were regularly intervened and were followed up regularly at 2 weeks, 4 weeks, 3 months, and 6 months. Active interventions in the form of awareness lectures, focused group discussions, and if needed, pharmacotherapy (nicotine/non-nicotine replacement therapy) was carried out for all participants. The outcome was assessed as no change, harm reduction (>50% reduction), complete cessation, and drop out. Statistical analysis of the data was done using the Statistical Package for the Social Sciences version 21.0. RESULTS: At the end of 1 month, there was higher tobacco cessation rate in the workplace group versus TCC group (n = 22, 44% vs n = 9, 18%; P < 0.0001). The tobacco cessation rate was maintained even after 6 months of intervention (n = 30, 60% vs n = 12, 24%; P = 0.002) and dropout rate was also lower among the workplace group than the TCC group (n = 14, 28% vs n = 27, 54%; P < 0.0001). CONCLUSIONS: Our study findings suggest that the workplace setting has superior outcome in tobacco cessation and harm reduction than clinical setting. In addition, it is associated with low dropout rate and the cessation effect is maintained over a period of 6 months.