Discovery and Optimization of N-Arylated Tetracyclic Dicarboximides That Target Primary Glioma Stem-like Cells.

We recently discovered a novel N-aryl tetracyclic dicarboximide MM0299 () with robust activity against glioma stem-like cells that potently and selectively inhibits lanosterol synthase leading to the accumulation of the toxic shunt metabolite 24(),25-epoxycholesterol. Herein, we delineate a systematic and comprehensive SAR study that explores the structural space surrounding the N-aryl tetracyclic dicarboximide scaffold. A series of 100 analogs were synthesized and evaluated for activity against the murine glioma stem-like cell line Mut6 and for metabolic stability in mouse liver S9 fractions.

Health service utilization and adherence to medication for hypertension and diabetes among Syrian refugees and affected host communities in Lebanon.

Methods: This study uses data from a 2015 household survey of Syrian refugees and Lebanese host communities. A total of 1,376 refugee and 686 host community households were surveyed using a cluster design with probability proportional to size sampling. Differences in outcomes of interest by population group were examined using Pearson's chi-square and t-test methods and the crude and adjusted odds of care-seeking and interrupted medication adherence among Syrian refugees were estimated using logistic regression.

Motivational factors for choosing treatment destinations among the patients treated overseas from the United Arab Emirates: results from the knowledge, attitudes and perceptions survey 2012.

Background: Travelling seeking healthcare is becoming common phenomenon. There is limited research to understand factors associated with destinations of choice. Each year the Dubai Health Authority (DHA) spends millions of dollars to cover Emiratis seeking healthcare overseas.

Treatment destinations and visit frequencies for patients seeking medical treatment overseas from the United Arab Emirates: results from Dubai Health Authority reporting during 2009-2016.

Background: Each year, the Dubai Health Authority (DHA) spends millions of dollars to cover the costs of United Arab Emirates (UAE) nationals seeking healthcare overseas. Patients may travel overseas to seek an array of treatments. It is important to analyze the number of trips and treatment destinations for patients travelling overseas to provide baseline information for the DHA to improve polices and strategies related to overseas treatment for UAE nationals.

Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC).

Despite advances in targeted anticancer therapies, there are still no small-molecule-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small molecule that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chemistry evaluation of a collection of TASIN analogues and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity.