Pyrazine is one of the important class of heterocyclic compounds that can be obtained naturally or synthesized chemically. Pyrazine ring has got importance in exhibiting various biological activities in association with other scaffolds like pyrrole, pyrazole, imidazole, triazole, tetrazole, thiophene, oxazole, pyridine, piperidine and piperazine. Presence of pyrazine ring as a basic scaffold in various clinically used drugs exhibits its importance in drug design. In this review, attempt has been made to disclose various therapeutic applications of pyrazine derivatives reported during the last decade.
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http://dx.doi.org/10.2174/1389557511313110007 | DOI Listing |
J Hematol Oncol
December 2024
Experimentelle Unfallchirurgie (ForMED), Justus-Liebig-Universität Gießen, Aulweg 128, 35392, Gießen, Germany.
Background: Accumulation of malignant plasma cells in the bone marrow causes lytic bone lesions in 80% of multiple myeloma patients. Frequently fracturing, they are challenging to treat surgically. Myeloma cells surviving treatment in the presumably protective environment of bone lesions impede their healing by continued impact on bone turnover and can explain regular progression of patients without detectable minimal residual disease (MRD).
View Article and Find Full Text PDFJ Cell Mol Med
December 2024
Menarini Group, Preclinical and Translational Sciences, Pomezia, Rome, Italy.
MEN1703 is a first-in-class, oral, Type I dual PIM/FMS-like tyrosine kinase 3 inhibitor (FLT3i) investigated in a Phase I/II DIAMOND-01 trial in patients with acute myeloid leukaemia (AML). Gilteritinib is a highly potent and selective oral FLT3i approved for the treatment of relapsed/refractory AML with FLT3 mutations. Although gilteritinib showed strong single-agent activity in FLT3-mutated AML, the development of gilteritinib resistance limits response durability, indicating the importance of novel combination strategies to improve disease outcome.
View Article and Find Full Text PDFCell Biol Toxicol
November 2024
Suzhou Medical College of Soochow University, Suzhou City, 215123, Jiangsu Province, P.R. China.
Background: Gilteritinib is a commonly used targeted drug for acute myeloid leukemia (AML), but the emergence of gilteritinib resistance greatly reduces the therapeutic effect. RING finger protein 38 (RNF38), a protein with RING Finger domain and E3 ubiquitin ligase activity, has been implicated in tumorigenesis and drug resistance. However, the role and mechanism of RNF38 in the gilteritinib resistance of AML remains unclear.
View Article and Find Full Text PDFJ Am Chem Soc
December 2024
Department of Chemistry, Faculty of Pure and Applied Sciences, University of Tsukuba, Tsukuba, Ibaraki 305-8571, Japan.
We have developed photocatalytic oxidation of aromatic substrates using O as a terminal oxidant to afford only 2e-oxidized products without the reductive activation of O in acidic water under visible-light irradiation. A Ru complex () bearing a pyrazine moiety as the active site in tetrapyrido[3,2-:2',3'-:3″,2″-:2‴,3‴-]phenazine (tpphz) as a ligand was employed as a photocatalyst. The active species for the photocatalysis was revealed to be not complex itself but the protonated form, -H, protonated at the vacant diimine site of tpphz.
View Article and Find Full Text PDFHeliyon
October 2024
Department of Chemistry, University of Liverpool, UK.
Millions of lives have been lost to the deadly SARS-CoV-2 virus. Vaccines and antiviral drugs are essential scientific tools in combating viral infections. This study focused on the RdRp inhibitor favipiravir, exploring new analogs by substituting the fluorine atom on the pyrazine ring with both homocyclic and heterocyclic moieties.
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