The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.

Glycogen synthase kinase 3β (GSK 3β) is a highly conserved serine/threonine kinase, and its roles in cancer remain controversial. Cumulative evidence supported that GSK 3β inhibitors could suppress ovarian cancer (OC) development in vitro and made a new direction for ovarian cancer treatment. Here, we reported a series of novel substituted benzothiazinones as non-ATP competitive inhibitors of GSK 3β.

[Design and synthesis of 3'-methyl-furanonucleosides and their anti-tumor activities].

Taking 3'-Me-Ado (3'-methyladenosine) and Cladribine as the leading compounds, seventeen 3'-C-methyl-furanonucleosides were designed and synthesized. All the structures were confirmed by 1H NMR and MS. The target compounds were tested in vitro against human pulmonary carcinoma A549, human colon carcinoma LOVO and human leukemia CEM by MTT assay.

[Synthesis and antibacterial activities of 7-{4-[2-[2-substituted-4-((5S)-5-acetylaminomethyl-2-oxo-oxazolidin-3-yl)}-phenyl] -ethyl]-piperazin-1-yl}-fluoroquinolones].

Aim: To find out new oxazolidinone-fluoroquinolone derivatives with high antibacterial activity.

Methods: Some 7-{4-[2-[2-substituted-4-((5S)-5- acetylaminomethyl-2-oxo-oxazolidin-3-yl)-phenyl]-ethyl]-piperazin-1-yl}-fluoroquinolones were designed and synthesized, and their antibacterial activities were tested in vitro.

Results: Twenty target compounds were obtained and their structures were confirmed by 1H NMR and MS.

[Synthesis and antibacterial activity of (S) -5-acetylaminomethyl-3-[(4-substituted-aminomethyl) phenyl] -2-oxazolindinone derivatives].

Aim: To synthesize oxazolindinone derivatives and test their antibacterial activities.

Methods: 3-Halo-4-methylaniline was acylated with benzyl chloroformate, followed by cyclization with (R)-glycidyl butyrate, acylation with methanesulfonyl chloride, substitution with NaN3, reduction with H2 + Pd/C or P(OMe)3 + HCl, acylation with Ac2O, and bromination with NBS to form bromides VIIIa and VIIIb, Substitution of the bromides with various amines including aliphatic amine and aromatic amine provided the target compounds IXa and IXb. The in vitro antibacterial activity of the target compounds was tested.