Thieno[2,3‐d]pyrimidines in the Synthesis of Antitumor and Antioxidant Agents |
| |
| Authors: | Ashraf A. Aly Alan B. Brown Mohamed Ramadan Amira M. Gamal‐Eldeen Mohamed Abdel‐Aziz Gamal El‐Din A. A. Abuo‐Rahma Mohamed F. Radwan |
| |
| Affiliation: | 1. Chemistry Department, Florida Institute of Technology, Melbourne, FL, USA;2. Department of Medicinal Chemistry, Faculty of Pharmacy, El‐Minia University, El‐Minia, Egypt;3. Department of Biochemistry, Division of Genetic Engineering and Biotechnology, National Research Centre, Dokki, Giza, Egypt |
| |
| Abstract: | Dimethyl acetylenedicarboxylate, ethyl propiolate, and E‐dibenzoylethylene react with thienopyrimidines (cyclo‐pentyl, ‐hexyl, and ‐heptyl) derivatives to form thiazolo[3,2‐a]thieno‐[2,3‐d]pyrimidin‐2‐ylidene) acetates, thieno[2,3‐d]pyrimidin‐2‐ylthioacrylates, and thieno[2′,3′:4,5]pyrimido[2,1‐b][1,3]thiazin‐6‐ones, respectively. Reactions proceed via cyclization and thio‐addition processes. Some derivatives of thienopyrimidines showed high inhibition of Hep‐G2 cell growth compared with the growth of untreated control cells. However, the fused heptyl of thienopyrimidothiazines indicates a promising specific antitumor agent against Hep‐G2 cells with IC50 < 20 μM. |
| |
| Keywords: | Antitumor activity Cyclization Dimethyl acetylenedicarboxylate E‐Dibenzoylethylene Thienopyrimidines |
|
|
