868563-96-6Relevant academic research and scientific papers
Design, synthesis and evaluation of novel thienopyridazine derivatives as Chk1/2 inhibitors
Liu, Hanyu,Qian, Feng,Shen, Dadong,Wang, Pu
, (2022/03/07)
In order to search for novel checkpoint kinase 1/2 (Chk1) inhibitors, we have designed and synthesized a series of new compounds incorporating thienopyridazine core. Bioevaluation showed that compounds 10j, 10i, 13e and 10o exhibited relatively good inhibitory activity. Notably, compound 10o displayed high selectivity against a panel of kinases and inhibited Chk1/2 signaling pathway stimulated by DNA damage drugs in cellular level. Molecular docking of 10o to the ATP-binding site of Chk1 kinase domain indicated the existence of polar interactions between 10o and the ATP-ribose-binding residues of Chk1. In mouse HT-29 xenografts, a synergistic effect was observed. Co-treatment by CPT-11 and 10o significantly diminished the tumor volume, indicating the great potential of 10o as a candidate of Chk1/2 inhibitor.
Rhodium Thiavinyl Carbenes from 1,2,3-Thiadiazoles Enable Modular Synthesis of Multisubstituted Thiophenes
Kurandina, Daria,Gevorgyan, Vladimir
supporting information, p. 1804 - 1807 (2016/05/19)
The rhodium-catalyzed transannulation reaction between 1,2,3-thiadiazoles and alkynes, proceeding via intermediacy of the previously unknown Rh thiavinyl carbene, toward a highly efficient and regioselective synthesis of up to fully substituted thiophenes is described.
THIENOPYRIDAZINES AS IKK INHIBITORS
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Page/Page column 26-27, (2008/06/13)
The invention is concerned with a compound of formula (I): or a pharmaceutically acceptable salt, a solvate or a prodrug thereof, wherein A, Y, Z and Rl are as defined in the description and the claims. These compounds inhibit IKK and can be used as medicaments.
