Estrogen receptor beta (ERβ) selective ligands have attracted much attention recently in the design of anti-cancer drugs that are devoid of the common side effects of estrogen. Structural studies of estrogen receptor alpha (ERα) and β revealed that there were considerable differences in their ligand-binding cavity and in their volume. Hence, the present study has hypothesized that size and shape descriptors can influence the affinity/selectivity of the ligands towards ERβ. To prove the same, quantitative structure-activity relationship (QSAR) analyses were carried out using multiple regression analysis on 2-phenylquinoline, tetrahydrofluorenone and 3-hydroxy-6H-benzo[c]chromen-6-one series. Results indicate that increased lipophilicity, decrease in ellipsoidal volume and width of substituents, presence of halogen atoms was essential for the ligands to have high affinity/selectivity towards ERβ. QSAR models obtained were both internally and externally validated. The study delineates that the size and shape descriptors are best modulators of ERβ affinity/selectivity. Docking studies were performed to support our QSAR results.
Background: Most common cause of death in developed and developing countries is oral cancer, with increasing habits of smoking, tobacco chewing, and alcohol consumption. Early diagnosis required for better cure rates and improves the quality of life. Screening of oral cancer in general hospitals provides a "window of opportunity" for early diagnosis. Aim: To assess the knowledge of oral cancer and the screening practice among medical students in Chennai city. Objective: To investigate whether medical students are aware of the risk factors and clinical signs of oral cancer. Methodology: A total of 500 medical students (365 undergraduate and 165 postgraduate) studying in Chennai city were included in the questionnaire based survey. Results: About 50% of medical students are aware of oral cancer and only 37% of students screen patients for oral signs during examination; 65.8% of students accept tobacco to be the main etiology of cancer; 31.2% of students accept buccal mucosa to be the common site, and 83% of students are willing to participate in oral cancer screening program.
Conclusion:The prognosis of patients depends on the stage of the disease at the time of diagnosis.
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