Antitumor agents. Part 226:( dagger ) synthesis and cytotoxicity of 2-Phenyl-4-quinolone acetic acids and their esters.

Xia Y; Yang ZY; Xia P; Bastow KF; Nakanishi Y; Nampoothiri P; Hamel E; Brossi A; Lee KH

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Antitumor agents. Part 226:( dagger ) synthesis and cytotoxicity of 2-Phenyl-4-quinolone acetic acids and their esters.

机译：抗肿瘤药。第226部分：(匕首）2-苯基-4-喹诺酮乙酸及其酯的合成和细胞毒性。

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2-Phenyl-4-quinolone acetic acids and their esters were synthesized and evaluated for interaction with tubulin and for cytotoxicity against a panel of human tumor cell lines. 2-Phenyl- and 2-(2'-fluorophenyl)-4-quinolone-8-acetic acids (11 and 12) displayed potent cytotoxicity with ED(50) values at nanomolar concentrations, but had minimal activity against tubulin polymerization. 2-(2'-Fluorophenyl)-4-quinolone-6-acetic acid (3) and 2-(2'-fluorophenyl)-4-quinolone-8-acetic acid methyl ester (10) moderately inhibited tubulin polymerization.

机译：合成了2-苯基-4-喹诺酮乙酸及其酯，并评估了其与微管蛋白的相互作用以及对一组人类肿瘤细胞系的细胞毒性。 2-苯基和2-（2'-氟苯基）-4-喹诺酮-8-乙酸（11和12）在纳摩尔浓度下显示出强的细胞毒性和ED（50）值，但对微管蛋白聚合的活性却最小。 2-（2'-氟苯基）-4-喹诺酮-6-乙酸（3）和2-（2'-氟苯基）-4-喹诺酮-8-乙酸甲酯（10）适度抑制微管蛋白聚合。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2003年第17期|共3页
作者
Xia Y; Yang ZY; Xia P; Bastow KF; Nakanishi Y; Nampoothiri P; Hamel E; Brossi A; Lee KH;
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正文语种 eng
中图分类基础医学;
关键词
Quinolones; Acetic Acid; Cytotoxicity; Tubulin; 喹诺酮类; 醋酸; 微管蛋白;

机译：Quinolones;Acetic Acid;Cytotoxicity;Tubulin;喹诺酮类;醋酸;微管蛋白;

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1. Antitumor agents. Part 226:( dagger ) synthesis and cytotoxicity of 2-Phenyl-4-quinolone acetic acids and their esters. [J] . Xia Y, Yang ZY, Xia P, Bioorganic and Medicinal Chemistry Letters . 2003,第17期

机译：抗肿瘤药。第226部分：(匕首）2-苯基-4-喹诺酮乙酸及其酯的合成和细胞毒性。
2. Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents. [J] . Xia Y, Yang ZY, Xia P, Journal of Medicinal Chemistry . 2001,第23期

机译：抗肿瘤剂。 211.氟化的2-苯基-4-喹诺酮衍生物作为抗有丝分裂的抗肿瘤剂。
3. Antitumor agents. 271: total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents. [J] . Yen CT, Nakagawa Goto K, Hwang T Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：抗肿瘤剂。 271：含有抗炎和细胞毒剂的碱和类似物的总合成和评价。
4. Novel Angular Furoquinolinone Bearing Flexible Chain as Antitumor Agent: Design, Synthesis, Cytotoxic Evaluation and Studies on DNA-Binding [C] . The 12th Asian Pacific Confederation of Chemical Engineering Congress(第十二届亚太化工联盟大会暨化工展览会)论文集 . 2008

机译：新型角形呋喃喹啉酮具有柔性链作为抗肿瘤剂：设计，合成，细胞毒评价和DNA结合研究。
5. Synthesis and decarboxylative coupling of sulfonyl acetic esters. [D] . Weaver, Jimmie Dean, III. 2010

机译：磺酰基乙酸酯的合成和脱羧偶联。
6. Antitumor Agents. 271. Total Synthesis and Evaluation of Brazilein and Analogs as Anti-inflammatory and Cytotoxic Agents [O] . Chiao-Ting Yen, Kyoko Nakagawa-Goto, Tsong-Long Hwang, -1

机译：抗肿瘤剂。 271.含有抗炎和细胞毒性剂的碱性合成和评价和评价
7. Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents [O] . Chiao-Ting Yen, Kyoko Nakagawa-Goto, Tsong-Long Hwang, 2010

机译：抗肿瘤剂。 271：含有抗炎和细胞毒剂的碱性合成和评价和评价

Antitumor agents. Part 226:( dagger ) synthesis and cytotoxicity of 2-Phenyl-4-quinolone acetic acids and their esters.

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