Synthesis and In Vitro Antiproliferative Activity of Novel Phenyl Ring-Substituted 5-Alkyl-12(H)-quino[3,4-b][1,4]benzothiazine Derivatives
Copyright policy )Synthesis and In Vitro Antiproliferative Activity of Novel Phenyl Ring-Substituted 5-Alkyl-12(H)-quino[3,4-b][1,4]benzothiazine Derivatives
A novel series of tetracyclic quinobenzothiazine derivatives was synthetized. Compounds containing a substituent (hydroxyl, methyl, phenyl, piperidyl, or piperazinyl) in positions 9 and 11 were obtained by cyclization of suitable 4-aminoquinolinium-3-thiolates. Quinobenzothiazine 10-O-substituted derivatives were obtained by alkylating the hydroxyl group in position 10 of the parent (quinobenzothiazine) system. Antiproliferative activity of the synthesized compounds was studied using cultured neoplastic cells (MDA-MB-231, SNB-19, and C-32 cell lines). Four selected compounds were investigated in more detail for cytotoxicity and antiproliferative effect. Transcriptional activity of genes regulating cell cycle (TP53), apoptosis (BAX, BCL-2), as well as proliferation (H3) were assessed. Finally, the ability of the selected compounds to bind DNA was checked in the presence of ethidium bromide.
Molecular Structure, Cell Survival, Cell Cycle, Thiazines, phenothiazine, cisplatin, Organic chemistry, Antineoplastic Agents, Apoptosis, anticancer, phenothiazine; azaphenothiazine; anticancer; cisplatin, Article, Gene Expression Regulation, Neoplastic, Structure-Activity Relationship, QD241-441, azaphenothiazine, Cell Line, Tumor, Humans, Drug Screening Assays, Antitumor, Tumor Suppressor Protein p53, Cell Proliferation, bcl-2-Associated X Protein
Molecular Structure, Cell Survival, Cell Cycle, Thiazines, phenothiazine, cisplatin, Organic chemistry, Antineoplastic Agents, Apoptosis, anticancer, phenothiazine; azaphenothiazine; anticancer; cisplatin, Article, Gene Expression Regulation, Neoplastic, Structure-Activity Relationship, QD241-441, azaphenothiazine, Cell Line, Tumor, Humans, Drug Screening Assays, Antitumor, Tumor Suppressor Protein p53, Cell Proliferation, bcl-2-Associated X Protein
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