Design and synthesis of thieno[2,3-d]pyrimidine derivatives and their biological evaluation as Antitumor and anti-HIV agents / Ramy Sayed Aboelella Ahmed ; Supervised Fatma Abdelfattah Ragab , Sahar Mahmoud Abouseri , Diaa Abdelsamei

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

In a search for new cytotoxic agents with improved anticancer profile, some new thienopyrimidine and thienotriazolopyrimidine derivatives were synthesized. All the synthesized compounds are tested for their in-vitro cytotoxicity against human breast cancer cell line (MCF-7) in which tyrosine kinases are highly expressed. All target compounds are then subjected for further evaluation against receptor tyrosine kinase enzymes; namely, epidermal growth factor receptor (EGFR), (ErbB-2) and vascular endothelial growth factor receptor-2 (VEGFR-2).Compounds in series I were designed to be nonnucleoside reverse transcriptase inhibitors (NNRTIs). Compounds Va-f were assayed for their inhibitory activity against HIV-1 (IIIB strain) and HIV-2 (ROD strain) using nevirapine as a reference inhibitor. They were found to be moderately active against reverse transcriptase

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