Synthesis of substituted benzylamino- and heterocyclylmethylamino carbodithioate derivatives of 4-(3H)-quinazolinone and their cytotoxic activity.

Cao SL; Feng YP; Zheng XL; Jiang YY; Zhang M; Wang Y; Xu M

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Synthesis of substituted benzylamino- and heterocyclylmethylamino carbodithioate derivatives of 4-(3H)-quinazolinone and their cytotoxic activity.

机译：4-（3H）-喹唑啉酮的取代的苄基氨基和杂环基甲基氨基碳二硫代酸酯衍生物的合成及其细胞毒性活性。

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摘要

A new series of substituted benzylamino- and heterocyclylmethylamino carbodithioate derivatives of 4-(3H)-quinazolinone were synthesized via four steps starting from 2-amino-5-methylbenzoic acid and initially screened against A-549 (human non-small cell lung cancer), HCT-8 (human colon cancer), and Bel-7402 (human liver cancer) cell lines at the single concentration of 5 microg/mL using the colorimetric MTT assay. The IC50 values were determined for the compounds reaching > or = 70% inhibition in primary screening by serial dilution. Among the newly synthesized compounds, 9n exhibited potent in vitro cytotoxicity against A-549, HCT-8, and Bel-7402 cell lines with the IC50 values of 1.65, 0.93, and 1.43 microM, respectively.

机译：从2-氨基-5-甲基苯甲酸开始，通过四个步骤合成了一系列新的4-（3H）-喹唑啉酮的取代苄氨基-和杂环基甲基氨基碳二硫代酸酯衍生物，并初步针对A-549（人类非小细胞肺癌）进行了筛选使用比色MTT分析法检测单个浓度为5 microg / mL的HCT-8，HCT-8（人类结肠癌）和Bel-7402（人类肝癌）细胞系。测定通过系列稀释在初步筛选中达到>或= 70％抑制的化合物的IC50值。在新合成的化合物中，9n对A-549，HCT-8和Bel-7402细胞系表现出强大的体外细胞毒性，IC50值分别为1.65、0.93和1.43 microM。

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来源
《Archiv der Pharmazie》 |2006年第5期|共5页
作者
Cao SL; Feng YP; Zheng XL; Jiang YY; Zhang M; Wang Y; Xu M;
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正文语种 eng
中图分类药学;
关键词
Antineoplastic Agents; Quinazolines; 抗肿瘤药; 喹唑啉类;

机译：Antineoplastic Agents;Quinazolines;抗肿瘤药;喹唑啉类;

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1. Synthesis of substituted benzylamino- and heterocyclylmethylamino carbodithioate derivatives of 4-(3H)-quinazolinone and their cytotoxic activity. [J] . Cao SL, Feng YP, Zheng XL, Archiv der Pharmazie . 2006,第5期

机译：4-（3H）-喹唑啉酮的取代的苄基氨基和杂环基甲基氨基碳二硫代酸酯衍生物的合成及其细胞毒性活性。
2. Synthesis of new 3-(3-phenyl-isoxazol-5-yl) or 3-((3-phenyl-isoxazol-5-yl)-amino) substituted 4(3H)-quinazolinone derivatives with antineoplastic activity. [J] . Raffa D, Daidone G, Schillaci D, Die Pharmazie . 1999,第4期

机译：具有抗肿瘤活性的新的3-（3-苯基-异恶唑-5-基）或3-（（3-苯基-异恶唑-5-基）-氨基）取代的4（3H）-喹唑啉酮衍生物的合成。
3. Synthesis of new 3-(3-phenyl-isoxazol-5-yl) or 3-((3-phenyl-isoxazol-5-yl)-amino) substituted 4(3H)-quinazolinone derivatives with antineoplastic activity. [J] . Raffa D, Daidone G, Schillaci D, Die Pharmazie . 1999,第4期

机译：具有抗肿瘤活性的新的3-（3-苯基-异恶唑-5-基）或3-（（3-苯基-异恶唑-5-基）-氨基）取代的4（3H）-喹唑啉酮衍生物的合成。
4. Structure-activity relationships of herbicidal 3-phenyl substituted derivatives of 1,2,3-benzotriazin-4-ones, 4(3H)-quinazolinones, and 2,4(1H,3H)-quinazolinediones [C] . B Li, H Z Yang British Crop Protection Council International Congress of the Crop Science and Technology . 2003

机译：三苯并三苯基-4-氮，4（3H） - 喹唑啉酮和2,4（1H，3H） - 喹唑啉代唑啉代唑啉代唑啉代唑啉代唑啉代唑啉代唑（2,3-苯并三苯基-4-苯基取代衍生物）的结构 - 活性关系
5. Synthesis and characterization of some new 4(3H)-quinazolinones. [D] . Schmidt, Duran Scott. 1997

机译：某些新型4（3H）-喹唑啉酮的合成与表征。
6. Synthesis and Antiviral Bioactivities of 2-Aryl- or 2-Methyl-3-(substituted- Benzalamino)-4(3H)-quinazolinone Derivatives [O] . Xingwen Gao, Xuejian Cai, Kai Yan, 2007

机译：2-芳基或2-甲基-3-（取代的苯甲氨基）-4（3H）-喹唑啉酮衍生物的合成及抗病毒活性
7. QSAR analysis of substituted benzylamino- and heterocyclylmethylamino-carbodithioate derivatives of 4-(3H)-quinazolinone using CoMFA and SCORE2.0 [O] . Liu Feng, Liu ShiYing, Liu Yan, 2007

机译：使用CoMFA和SCORE2.0对4-（3H）-喹唑啉酮的取代的苄基氨基和杂环基甲基氨基碳二硫代酸酯衍生物进行QSAR分析

Synthesis of substituted benzylamino- and heterocyclylmethylamino carbodithioate derivatives of 4-(3H)-quinazolinone and their cytotoxic activity.

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