Browsing by Author "Shahin, Inas G"
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Item Development of Semisynthetic Apoptosis-Inducing Agents Based on Natural Phenolic Acids Scaffold: Design, Synthesis and In-Vitro Biological Evaluation(Multidisciplinary Digital Publishing Institute (MDPI), 2022-10) Ezzat, Shahira M; Teba, Heba El Sayed; Shahin, Inas G; Hafez, Ahmed M; Kamal, Aliaa M; Aborehab, Nora M: A crucial target in drug research is magnifying efficacy and decreasing toxicity. Therefore, using natural active constituents as precursors will enhance both safety and biological activities. Despite having many pharmacological activities, caffeic and ferulic acids showed limited clinical usage due to their poor bioavailability and fast elimination. Therefore, semisynthetic compounds from these two acids were prepared and screened as anticancer agents. In this study, CA and FA showed very potent anticancer activity against Caco-2 cells. Consequently, eighteen derivatives were tested against the same cell line. Four potent candidates were selected for determination of the selectivity index, where compound 10 revealed a high safety margin. Compound 10 represented a new scaffold and showed significant cytotoxic activity against Caco-2. Cell-cycle analysis and eval- uation of apoptosis showed that derivatives 10, 7, 11, 15 and 14 showed the highest proportion of cells in a late apoptotic stage. :Item Recent Advances in The Synthesis of Thiazole Ring: Mini Review(Bentham Science Publishers, 2022-04) Shahin, Inas G; Mohamed, Khaled Omar; Taher, Azza; Mayhoub, Abdelrahman S; Kassab, AsmaaThe thiazole scaffold is an essential structural foundation in a plethora of pharmaceutical products having an extensive array of biological activities. Consequently, its synthesis has been extensively discussed in the literature. In this mini review, we have summarized the recent advances of thiazole synthesis covering articles published between 2002 and 2021. We have reviewed and discussed variable recent and novel routes for the synthesis of compounds containing thiazole ring from various starting materials such as thiourea, thioamide or thiosemicarbazone. Additionally, we have illustrated environmentally benign methods for thiazole synthesis. We hope that this review can help other researchers in efficient synthesis of thiazole ring.