Synthesis and evaluation of spumigin analogues library with thrombin inhibitory activityŽula, Aleš (Avtor) Będziak, Izabela (Avtor) Kikelj, Danijel (Avtor) Ilaš, Janez (Avtor) marine productsnatural peptidespeptidomimeticsthrombin inhibitionSpumigins are marine natural products derived from cyanobacteria Nodularia spumigena, which mimics the structure of the D-Phe-Pro-Arg sequence and is crucial for binding to the active site of serine proteases thrombin and factor Xa. Biological evaluation of spumigins showed that spumigins with a (2S,4S)-4-methylproline central core represent potential lead compounds for the development of a new structural type of direct thrombin inhibitors. Herein, we represent synthesis and thrombin inhibitory activity of a focused library of spumigins analogues with indoline ring or L-proline as a central core. Novel compounds show additional insight into the structure and biological effects of spumigins. The most active analogue was found to be a derivative containing L-proline central core with low micromolar thrombin inhibitory activity.20182021-03-12 10:22:41Članek v reviji125357UDK: 577ISSN pri članku: 1660-3397DOI: 10.3390/md16110413COBISS_ID: 39787781OceCobissID: 23578841sl