| Modification of Monastrol with liphophilic diamondoid adamantane |
| کد مقاله : 1082-ICOC |
| نویسندگان |
|
حسین رستم زاده *، عادله مشتقی زنوز دانشگاه شهید مدنی آذربایجان |
| چکیده مقاله |
| Diamondoids are cage-like hydrocarbon molecules that can be described as nanometer- sized, hydrogen-terminated diamond hydrocarbons, also known as nanodiamonds [1]. Adamantane, with the formula C 10 H 16 , is the smallest diamondoid. Adamantane derivatives have found numerous applications in medicinal chemistry. There are eight adamantane-based drug now in clinical use for the treatment of neurodegenerative disorders, viral infections and type-2 diabetes. On the other hand, adamantane's lipophilic properties make it useful as a "liphophilic bullet" to modify existing drugs. Adamantane modifications are utilized in drug development to increase lipophilicity and stability. This enhancement improves the pharmacokinetics of drug and facilitates its passage through cell membranes [2]. Dihydropyrimidinones (DHPMs) have widespread pharmacological activities, and are regarded as one of the most important groups of drug-like scaffolds [3]. Monastrol, with a dihydropyrimidone scaffold, is a cell-permeable small molecule inhibitor that targets the mitotic kinesin Eg5, a motor protein essential for mitotic spindle bipolarity. Monastrol is a cell-permeable small molecule with a dihydropyrimidone (DHPM) scaffold that specifically inhibits the mitotic kinesin Eg5 protein. This inhibition leads to cell cycle arrest in mitosis. In this work, the novel adamantane-modified monastrol derivative was synthesized through the Biginelli reaction of adamantly-containing active methylene compound, 3-hydroxybenzaldehyde, and thiourea The structure of product was completely characterized using FT-IR, 1 H and 13 C NMR spectroscopy. |
| کلیدواژه ها |
| Monastrol, Diamondoid, Adamantane, Biginelli reaction |
| وضعیت: پذیرفته شده |