- Phenothiazine compound and application thereof
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The invention provides a phenothiazine compound and application thereof to preparation of drugs for curing breast cancer and melanoma. The phenothiazine compound has higher inhibitory activity on thebreast cancer cell MDA- MB- 231, SUM159, MCF- 7, SKBR- 3 and the melanoma cell A375 and B16BL6 than trifluoperazine and thioridazine, and can be applied to curing breast cancer and melanoma. The general formula of the phenothiazine compound is as following (the formula is shown in the description), wherein R1 and R2 are as shown in the description.
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Paragraph 0142-0146
(2019/06/07)
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- Repositioning of the antipsychotic trifluoperazine: Synthesis, biological evaluation and in silico study of trifluoperazine analogs as anti-glioblastoma agents
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Repositioning of the antipsychotic drug trifluoperazine for treatment of glioblastoma, an aggressive brain tumor, has been previously suggested. However, trifluoperazine did not increase the survival time in mice models of glioblastoma. In attempt to identify an effective trifluoperazine analog, fourteen compounds have been synthesized and biologically in vitro and in vivo assessed. Using MTT assay, compounds 3dc and 3dd elicited 4–5 times more potent inhibitory activity than trifluoperazine with IC50 = 2.3 and 2.2 μM against U87MG glioblastoma cells, as well as, IC50 = 2.2 and 2.1 μM against GBL28 human glioblastoma patient derived primary cells, respectively. Furthermore, they have shown a reasonable selectivity for glioblastoma cells over NSC normal neural cell. In vivo evaluation of analog 3dc confirmed its advantageous effect on reduction of tumor size and increasing the survival time in brain xenograft mouse model of glioblastoma. Molecular modeling simulation provided a reasonable explanation for the observed variation in the capability of the synthesized analogs to increase the intracellular Ca2+ levels. In summary, this study presents compound 3dc as a proposed new tool for the adjuvant chemotherapy of glioblastoma.
- Kang, Seokmin,Lee, Jung Moo,Jeon, Borami,Elkamhawy, Ahmed,Paik, Sora,Hong, Jinpyo,Oh, Soo-Jin,Paek, Sun Ha,Lee, C. Justin,Hassan, Ahmed H.E.,Kang, Sang Soo,Roh, Eun Joo
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p. 186 - 198
(2018/04/05)
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- The phenothiazine compound and its preparation method and application
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The invention relates to a phenothiazine compound and a preparation method thereof. The invention further relates the application of the phenothiazine compound in anti-cancer drug preparation and anti-cancer drugs using the compound as the effective component. The phenothiazine compound has the advantages that the compound with broad-spectrum anti-cancer effect is obtained by modifying phenothiazine ternary interlink parent nucleuses, synthesizing method is simple, and high yield is achieved; the phenothiazine compound has certain restraining effect on human breast cancer cells line MCF-7 and human hepatoma cell line Hep-G2, and a new thought is provided to new drugs satisfying clinic requirements.
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- Voltammetric determination of an antipsychotic agent trifluoperazine at a boron-doped diamond electrode in human urine
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A simple and efficient procedure is described for electrochemical determination of trifluoperazine (TFP), a prominent compound in a large group of phenothiazine derivatives with potent physiological activity. This method is based on the electrochemical oxidation of TFP in Britton-Robinson buffer solution in pH 6 at a boron-doped diamond electrode. Cyclic voltammetry provided a four well defined oxidation peaks at +0.65, +0.83, +1.06 and +1.35 V (vs. Ag/AgCl/3 M KCl electrode). Differential pulse voltammetry was applied as a very sensitive analytical technique for the determination of micromolar amounts of TFP. Two oxidation peaks on higher potentials were chosen for quantification of TFP. Under optimized conditions, the analytical curves obtained were linear in the TFP concentration range of 1.0 to 37.0 μmol L-1, with a detection limit of 0.7 and 0.6 μmol L-1, respectively. The effect of interfering agents (common urinary compounds) appeared to be negligible confirming the favourable selectivity of the method. The proposed method was analytically applied by determination of trifluoperazine content in model human urine samples with good accuracy (recoveries varied from 97% to 104%). The developed approach could be beneficial in analysis of TFP in biological samples using a boron-doped diamond electrode as an up-to-date electrochemical sensor and could represent an inexpensive analytical alternative to separation methods.
- Stankovi?,Dimitrijevi?,Kuzmanovi?,Krsti?,Petkovi?
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p. 107058 - 107063
(2016/01/08)
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- NOVEL COMPOSITIONS AND METHODS FOR TREATMENT OF DISEASES RELATED TO ACTIVATED LYMPHOCYTES
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The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.
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Page/Page column 56
(2008/06/13)
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