Synthesis, antitumor evaluation and molecular modeling studies of some new benzopyranone derivatives / Lina Mohamed Amin Abdelghany ; Supervised Sohair L. Elansary , Doaa E. Abdelrahman

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Nowadays, health is one of the most important domains that human beings have focused on in our society. Cancer is the biggest killer of our lives, so there is steadily increasing research in the field of anticancer therapy over recent years. However, lack of selectivity of chemotherapeutic agents against cancerous cells is still a significant problem with the current chemotherapy. Thus, in this study, forty eight coumarin derivatives were synthesized and forty compounds were selected for in vitro anticancer evaluation at NCI, USA. In addition, the most active compounds were subjected to IC50 calculations, cell cycle analysis, apoptosis induction and CDK2 enzyme inhibition assay. Furthermore, docking studies were undertaken for two compounds to gain insight into the possible binding mode of these compounds with the binding site of the CDK2 enzyme which is one of the enzymes involved in cell controlling and regulating cell cycle survival and proliferation through a number of downstream effectors

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