Design, synthesis and biological evaluations of 2-aminothiazole scaffold containing amino acid moieties as anti-cancer agents.

Due to the emerging mortality rate of colorectal cancer there is a high need for the management and control of this disease. Although several treatment approaches are being developed day by day yet the high incidence rate of colorectal cancer is still not controlled. To ease in the development of treatment therapies for colorectal cancer two derivatives of ethyl 2-aminothiazole 4-carboxylate were designed and synthesized. The compounds Ethyl 2-(2-(1,3-dioxoisoindolin-2-yl)acetamido)thiazole-4-carboxylate (5a) and ethyl 2-(2-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanamido)thiazole-4-carboxylate (5b) were characterized and studied for their anti-cancer activities. The in silico molecular modeling studies were performed against the target protein beta-catenin which is an important player in the progression of colorectal cancer. The in silico ADMET studies were performed to assess the basic physicochemical properties of these compounds. The in vitro antiproliferative assay and the enzyme inhibitory assay was performed to validate the role of these compounds in the colorectal cancer. The preliminary cytotoxic assay and the MTT assay of the compounds 5a and 5b against the colorectal cancer cell line HCT 116 showed 60% inhibition of cell proliferation with IC50 of 0.72µM and 1.55µM, respectively. The standard methotrexate showed IC50 of 0.7µM showing potent inhibitory action of these compounds. The in vitro validation of the anti-cancer effect of both compounds revealed significant inhibition of beta-catenin concentration at higher doses as compared to control. Both the in vitro and in vivo assays of compounds showed effective anti-cancer activities and depicts the future potential of these compounds in colorectal cancer.

Assessment of the risk factors of hypertension among adult & elderly group in twin cities of Pakistan.

OBJECTIVE: To estimate the prevalence of hypertension and to explore the risk factors associated with it. METHODS: In a cross-sectional study, a population based survey was conducted on inhabitants of Rawalpindi-Islamabad region, 219 individuals; aged 18 years or above were included in the study. Blood pressure was measured along with information about individual's demographic and socio-economic characteristics were obtained using a standard questionnaire.. RESULTS: Overall prevalence of hypertension was 29.22% (males: 21.9% and females: 78.1%) in individuals residing in Rawalpindi-Islamabad. High blood pressure is more associated with obesity (59.4%) and a progressive increase in hypertension was observed with increasing age. Bivariate analysis revealed that hypertension has a significant correlation (p-value<0.05) with age, gender, family status, weight and physical health. CONCLUSIONS: The study concludes that our generation is well aware about the risks and consequences of hypertension, but they still continue to make no or little effort in managing or preventing it. The factors contributing to hypertension are low physical activity, diet and lack of interest to maintain their health.