Synthesis and in vitro antiproliferative activity of 5-alkyl-12(H)-quino(3,4-b) (1,4)benzothiazinium salts.

Zieba A; Sochanik A; Szurko A; Rams M; Mrozek A; Cmoch P

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Synthesis and in vitro antiproliferative activity of 5-alkyl-12(H)-quino(3,4-b) (1,4)benzothiazinium salts.

机译：5-烷基-12（H）-喹啉（3,4-b）（1,4）苯并噻嗪鎓盐的合成及体外抗增殖活性。

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A novel method of synthesizing 1,4-thiazine ring has led to the series of 5-alkyl-12(H)-quino[3,4-b][1,4]benzothiazinium salts. The derivatives containing a butyl or decyl substituents on the quinoline nitrogen atom were obtained by alkylation of 12(H)-quino[3,4-b][1,4]benzothiazine with alkyl bromides. Antiproliferative activity in vitro of the compounds (3) was assessed using two cancer cell lines (Hct116 and LLC) and doxorubicin as a reference. Most of the studied phenothiazine derivatives showed activity against both cell lines investigated (2.2-19.6 mug/mL concentration range). A structure-activity relationship was established. Only the compounds with substituents in the 11-position of the quinobenzothiazine ring did not exhibit activity against either cell line.

机译：合成1,4-噻嗪环的新方法导致了一系列的5-烷基-12（H）-喹[3,4-b] [1,4]苯并噻嗪鎓盐。通过用烷基溴将12（H）-喹[3,4-b] [1,4]苯并噻嗪烷基化，获得在喹啉氮原子上含有丁基或癸基取代基的衍生物。使用两种癌细胞系（Hct116和LLC）和阿霉素作为参考评估了化合物（3）的体外抗增殖活性。大部分已研究的吩噻嗪衍生物均对所研究的两种细胞系均具有活性（2.2-19.6杯/毫升浓度范围）。建立了构效关系。仅在喹啉苯并噻嗪环的11位具有取代基的化合物不显示针对任一细胞系的活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第11期|共7页
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Zieba A; Sochanik A; Szurko A; Rams M; Mrozek A; Cmoch P;
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1. Synthesis and in vitro antiproliferative activity of 5-alkyl-12(H)-quino(3,4-b) (1,4)benzothiazinium salts. [J] . Zieba A, Sochanik A, Szurko A, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

机译：5-烷基-12（H）-喹啉（3,4-b）（1,4）苯并噻嗪鎓盐的合成及体外抗增殖活性。
2. Synthesis and in vitro antiproliferative activity of 5-alkyl-12(H)-quino(3,4-b) (1,4)benzothiazinium salts. [J] . Zieba A, Sochanik A, Szurko A, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

机译：5-烷基-12（H）-Quino（3,4-B）（1,4）苯并噻嗪盐的合成和体外抗增殖活性。
3. Synthesis and In Vitro Antiproliferative Activity of Novel Phenyl Ring-Substituted 5-Alkyl-12(H)-quino[3,4-b][1,4]benzothiazineDerivatives [J] . Zieba Andrzej, Latocha Malgorzata, Sochanik Aleksander, Molecules . 2016,第11期

机译：新型苯基环取代的5-烷基-12（H）-喹[3,4-b] [1,4]苯并噻嗪衍生物的合成及体外抗增殖活性
4. Synthesis of tetra-and tripeptide analogs of Substance P fragments and their peptoid-peptide hybrids.Study of their antiproliferative activity in vitro [C] . Paraskevi Ch.Vakalopoulou, Helen M.Makrodouli, George P.Stavropoulos International Peptide Symposium;European Peptide Symposium . 2005

机译：物质P片段的四氢肽和三肽类似物的合成及其拟肽杂交种。其抗增殖活性在体外
5. SYNTHESIS AND SOLUTION PHASE SECONDARY ION MASS SPECTRAL STUDIES OF ANTINEOPLASTIC 1,4-BIS(2'-CHLOROETHYL)-1,4- DIAZABICYCLO(2.2.1)HEPTANE SALTS. [D] . GIESCHEN, DONALD PAUL. 1984

机译：抗肿瘤塑料1,4-双（2'-氯乙基）-1,4-二氮杂双环（2.2.1）庚烷盐的合成和溶液相二次离子质谱研究。
6. Synthesis and In Vitro Antiproliferative Activity of Novel Phenyl Ring-Substituted 5-Alkyl-12(H)-quino34-b14benzothiazine Derivatives [O] . Andrzej Zięba, Małgorzata Latocha, Aleksander Sochanik, 2016

机译：新型苯基环取代的5-烷基-12（H）-喹34-b 14苯并噻嗪衍生物的合成及体外抗增殖活性
7. Synthesis and In Vitro Antiproliferative Activity of Novel Phenyl Ring-Substituted 5-Alkyl-12(H)-quino[3,4-b][1,4]benzothiazine Derivatives [O] . Andrzej Zięba, Małgorzata Latocha, Aleksander Sochanik, 2016

机译：新型苯环取代的5-烷基-12（H） - 喹[3,4-b] [1,4]苯并噻嗪衍生物的合成和体外抗增殖活性

Synthesis and in vitro antiproliferative activity of 5-alkyl-12(H)-quino(3,4-b) (1,4)benzothiazinium salts.

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