A New Class of Semisynthetic Anthracycline Glycoside Antibiotics Incorporating a Squaric Acid Moiety

Ferenc Sztaricskai; Anita Sum; Erzsebet Roth; Istvan F.Pelyvas; Szabolcs Sandor

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A New Class of Semisynthetic Anthracycline Glycoside Antibiotics Incorporating a Squaric Acid Moiety

机译：新型半合成蒽环类糖苷类抗生素，结合了方酸部分

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Treatment of the squaric acid amide esters(7,9)of anthracycline glycoside antibiotics with aliphatic and aromatic primary and secondary amines,amino acids,peptides and aminodeoxy sugars furnished the new asymmetric diamides 16-19,25-30,32,34 and 38-40 in stereoselective reactions which do not require protecting group-manipulations.The IC_(50)=0.12 muM value measured for daunorubicin(1)on human leukemia(HL-60)cells is comparable to those obtained for the daunomycin-L-leucyl squaric acid diamide(30,IC_(50)=0.18 muM)and the corresponding D-galactosamine derivative(40,IC_(50)=0.22

机译：用脂肪族和芳香族伯和仲胺，氨基酸，肽和氨基脱氧糖处理蒽环类抗生素抗生素的方酸酰胺酯（7,9），提供了新的不对称双酰胺16-19、25-30、32、34和38在不需要保护基团操纵的立体选择性反应中为-40。柔红霉素（1）在人白血病（HL-60）细胞上测得的IC_（50）= 0.12μM值与从道诺霉素L-亮氨酰上获得的IC_（50）相当方酸二酰胺（30，IC_（50）= 0.18μM）和相应的D-半乳糖胺衍生物（40，IC_（50）= 0.22

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《The Journal of Antibiotics: An International Journal》 |2005年第11期|共11页
作者
Ferenc Sztaricskai; Anita Sum; Erzsebet Roth; Istvan F.Pelyvas; Szabolcs Sandor;
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正文语种 eng
中图分类药学;
关键词
anthracycline glycoside antibiotics; squaric acid amides; HL-60 activity;

机译：蒽环类抗生素;方酸酰胺;HL-60活性;

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1. A New Class of Semisynthetic Anthracycline Glycoside Antibiotics Incorporating a Squaric Acid Moiety [J] . Ferenc Sztaricskai, Anita Sum, Erzsebet Roth, The Journal of Antibiotics: An International Journal . 2005,第11期

机译：新型半合成蒽环类糖苷类抗生素，结合了方酸部分
2. Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties. [J] . Tevyashova A, Sztaricskai F, Batta G, Bioorganic and Medicinal Chemistry Letters . 2004,第18期

机译：蒽环类抗生素的方酸酰胺的形成。合成和细胞毒性。
3. Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties. [J] . Tevyashova A, Sztaricskai F, Batta G, Bioorganic and Medicinal Chemistry Letters . 2004,第18期

机译：蒽环类抗生素的方酸酰胺的形成。合成和细胞毒性。
4. Distinctive features of complexation of anthracycline antibiotic daunomycin with deoxyhexanucleotide d(GCATGC) in aqueous solution: 1D- and 2D-NMR analysis [C] . Valery I. Pahomov, Olga V. Rogova, Vladimir S. Volynkin, Spectroscopy of Molecules and Crystals . 2004

机译：蒽环类抗生素道诺霉素与脱氧六核苷酸d（GCATGC）在水溶液中络合的显着特征：1D和2D NMR分析
5. Synthesis of 4'-O-glycopyranosyl paromomycin aminoglycoside antibiotics: Influence of the glycoside on antiribosomal, antibacterial activity and utilization of electrospray ionization mass spectrometry to evaluate reactivity of glycosyl phosphate. [D] . Chen, Weiwei. 2014

机译：合成4'-O-甘露糖基糖基巴龙霉素氨基糖苷类抗生素：糖苷对抗核糖体，抗菌活性的影响以及电喷雾电离质谱法用于评估糖基磷酸酯的反应性。
6. The Isothiocyanato Moiety. An Ideal Protecting Group for Stereoselective Sialic Acid Glycoside Synthesis and Subsequent Diversification [O] . Appi Reddy Mandhapati, Dr. Salla Rajender, Jonathan Shaw, -1

机译：异硫氰酸根基。立体选择性唾液酸糖苷合成及其后续分散的理想保护基
7. A New Series of Glycopeptide Antibiotics Incorporating a Squaric Acid Moiety [O] . Sztaricskai, Ferenc, Batta, Gyula, Herczegh, Pál, 2017

机译：含有方酸部分的新系列糖肽类抗生素

A New Class of Semisynthetic Anthracycline Glycoside Antibiotics Incorporating a Squaric Acid Moiety

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