1394236-18-0Relevant academic research and scientific papers
Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors
Wolff, Benjamin,J?nsch, Niklas,Sugiarto, Wisely Oki,Frühschulz, Stefan,Lang, Maraike,Altintas, Rabia,Oehme, Ina,Meyer-Almes, Franz-Josef
, (2019/10/19)
Human histone deacetylase 8 (HDAC8) is a highly promising target for neuroblastoma and other types of cancer. Several HDAC inhibitors are approved for the treatment of special cancer subtypes or are evaluated in clinical trials. By far the most drugs or d
Concise synthesis and anti-HIV activity of pyrimido[1,2-c][1,3] benzothiazin-6-imines and related tricyclic heterocycles
Mizuhara, Tsukasa,Oishi, Shinya,Ohno, Hiroaki,Shimura, Kazuya,Matsuoka, Masao,Fujii, Nobutaka
supporting information; experimental part, p. 6792 - 6802 (2012/09/22)
3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is a virucidal heterocyclic compound active against various viruses, including HCV, HIV, and simian immunodeficiency virus. Using facile synthetic approaches that we developed for the synthesis of pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic derivatives, the parallel structural optimizations of the central 1,3-thiazin-2-imine core, the benzene part, and the cyclic amidine part of PD 404182 were investigated. Replacement of the 6-6-6 pyrimido[1,2-c][1,3] benzothiazin-6-imine framework with 5-6-6 or 6-6-5 derivatives led to a significant loss of anti-HIV activity, and introduction of a hydrophobic group at the 9- or 10-positions improved the potency. In addition, we demonstrated that the PD 404182 derivative exerts anti-HIV effects at an early stage of viral infection.
