茚並喹啉衍生物的設計、合成及抗腫瘤活性研究

《茚並喹啉衍生物的設計、合成及抗腫瘤活性研究》是嚴勝驕為項目負責人，雲南大學為依託單位的地區科學基金項目。

基本介紹

• 中文名：茚並喹啉衍生物的設計、合成及抗腫瘤活性研究
• 項目類別：地區科學基金項目
• 項目負責人：嚴勝驕
• 依託單位 ：雲南大學

科研成果

序號	標題	類型	作者
1	Cascade reaction synthesis of multisubstituted bicyclic pyridone derivatives	期刊論文	Dandan Zhu|Xiaoying Wang|Shengjiao Yan|Jun Lin|
2	An environmentally benign, mild, and catalyst-free reaction of quinones with heterocyclic ketene aminals in ethanol: site-selective synthesis of rarely fused [1,2-a]indolone derivatives via an unexpected anti-Nenitzescu strategy	期刊論文	Rui Yang|Xin-Rong Lin|Sheng-Jiao Yan|Jun Lin|
3	One Step Synthesis of Fluorine-containing Bicyclicpyridine Compounds	期刊論文	Yang, R.-X.|,Liu, X.-M.|Yan, S.-J.|Lin, J.|
4	Synthesis and evaluation of the antitumor activityof polyhalo acridone derivatives	期刊論文	Zeng, X.-H.|Sun, B.|Lan, M.-B.|Lin, J.|
5	Three-component domino reaction synthesis of highly functionalized bicyclic pyrrole derivatives	期刊論文	Xiao-Ying Wang|Dan-Dan Zhu|Sheng-Jiao Yan|Jun Lin|
6	Three-component stereoselective synthesis of spirooxindole derivatives	期刊論文	Ni, Hangchen|Fan, Juan|Yan, Shengjiao|Lin, Jun|
7	Synthesis of 2-nitroso heterocyclic ketene aminals with (E)-1-nitro-4-(2-nitrovinyl)-benzene as the nitrosating agent	期刊論文	Hao, X.-P.|Huang, R.|Yan, S.-J.|Lin, J.|
8	Regioselective synthesis of 9,10-dihydro-6H-chromeno[4,3-d]imidazo-[1,2-a]pyridin-6-one derivatives	期刊論文	Hao, Xiao-Pan|Yan, Sheng-Jiao|Huang, Rong|Lin, Jun|
9	Cascade Reaction of Isatins with Heterocyclic Ketene Aminals: Synthesisof Imidazopyrroloquinoline Derivatives	期刊論文	Shengjiao Yan|Ling Hu|Yongchao Wang|Jun Lin|
10	Silver(I)-mediated coupling reaction of heterocyclic ketene aminals (HKAs) with bis(phenylsulfonyl)sulfides to synthesis of benzenesulfonothioyl-HKAs	期刊論文	Huang, Rong|Yang, Li-Fen|Yan, Sheng-Jiao|Lin, Jun|
11	Regioselective construction of 1,3-diazaheterocycle fused [1,2-a][1,8]naphthyridine derivatives via cascade reaction of quinolines with heterocyclic ketene aminals: a joint experimental–computational approach	期刊論文	Sheng Jiao Yan|
12	Palladium(II)-catalyzed cyclization of heterocyclic ketene aminals with (E)-ethyl 2,3-diiodoacrylates: selective synthesis of bicyclic pyrroles and bicyclic pyridones	期刊論文	Xin-Rong Lin|Hong-You Zhu|Sheng-Jiao Yan|Jun Lin|
13	Construction of C(sp(2))-S and C(sp(2))-Se bonds via a silver(I)-mediated coupling reaction of heterocyclic ketene aminals with diaryl dichalcogenides	期刊論文	Liu, Zhi-Cheng|Fang, Li|Yan, Sheng-Jiao|Lin, Jun|
14	Highly Diastereoselective Convergent Synthesis of Polycyclic Pyrroles with Consecutive Quaternary Stereocenters: Cascade Construction of Multiple C-C and C-Hetero Bonds	期刊論文	Lin, Xin-Rong|Huang, Rong|Yan, Sheng-Jiao|Lin, Jun|
15	Synthesis of polyhalo 2-aryl-4-aminoquinazolines and 3-amino-indazoles as anti-cancer agents	期刊論文	Peng, Qiong|Fan, Yin-Xian|Zhang, Ji-Hong|Lin, Jun|
16	A Three-Component Catalyst-Free Approach to Regioselective Synthesis of Dual Highly Functionalized Fused Pyrrole Derivatives in Water-Ethanol Media: Thermodynamics versus Kinetics	期刊論文	Liu, Zhi-Cheng|Yang, Li-Fen|Yan, Sheng-Jiao|Lin, Jun|
17	Regioselective synthesis of pyrrolo[1,2-a]-imidazoles and imidazo[1,2-a]-pyridines	期刊論文	Ma, Y.-L.|Lin, X.-R.|Yan, S.-J.|Lin, J.|
18	Three-Component Synthesis of Indanone-Fused Spirooxindole Derivatives	期刊論文	Liu, Xi-Ming|Huang, Rong|Yan, Sheng-Jiao|Lin, Jun|
19	Three-component cascade reaction synthesis of polycyclic 1,4-dihydropyridine derivatives in water	期刊論文	Kai-Min Wang|Xin-Rong Lin|Sheng-Jiao Yan|Jun Lin|
20	Heterocyclic Ketene Aminals: Scaffolds for Heterocycle Molecular Diversity	期刊論文	Wang, Kai-Min|Yan, Sheng-Jiao|Lin, Jun|
21	Regioselective construction of 1,3-diazaheterocycle fused [1,2-a][1,8]naphthyridine derivatives via cascade reaction of quinolines with heterocyclic ketene aminals: a joint experimental-computational approach	期刊論文	Yang, Sheng-Jiao|Zhang, Ji-Hong|Yan, Sheng-Jiao|Lin, Jun|
22	Synthesis of fused polyhalogeno-7a-hydroxy-[1,2-a]indol-5-one derivatives	期刊論文	Hao, X.-P.|Lin, X.-R.|Yan, S.-J.|Lin, J.|
23	Three component solvent-free synthesis of 1H-pyrazol-5(4H)-one-based heterocyclic ketene aminal derivatives	期刊論文	Hao, Xiaopan|Jiang, Xiuyang|Yan, Shengjiao|Lin, Jun|
24	Novel Three-Component Stereoselective Synthesis of Spirooxindole Derivatives	期刊論文	Hangchen Ni|Juan Fan|Shengjiao Yan|Jun Lin|
25	Synthesis and antimicrobial activity of polyhalo isophthalonitrile derivatives	期刊論文	Neng-Qin He|Ya-Juan Tang|Xing-Hong Wang|Jun Lin|
26	Three Component Solvent-free Synthesis of Chroman-2,4-dione-based Heterocyclic Ketene Aminal (HKA) Derivatives by "GAP" Chemistry	期刊論文	Hao, Xiao-Pan|Jiang, Xiu-Yang|Yan, Sheng-Jiao|Lin, Jun|
27	異喹啉亞胺類化合物的合成	會議論文	-
28	Catalyst-free concise synthesis of imidazo[1,2-a]pyrrolo[3,4-e]pyridine derivatives	期刊論文	Zhu, Li|Fang, Li|Yan, Shengjiao|Lin, Jun|
29	Highly Diastereoselective Convergent Synthesis of Polycyclic Pyrroles with Consecutive Quaternary Stereocenters: Cascade Construction of Multiple C？C and C？Hetero Bonds	期刊論文	Xin-Rong Lin|Rong Huang|Sheng-Jiao Yan|Jun Lin|
30	Catalyst-free cascade reaction of heterocyclic ketene aminals with N-substituted maleimide to synthesise bicyclic pyrrolidinone derivatives	期刊論文	Zhang, Hai-Rui|Lin, Xin-Rong|Yan, Sheng-Jiao|Lin, Jun|
31	Three-component solvent-free synthesis of fluorine substituted bicyclic pyridines	期刊論文	Chen, X.-B.|Huang, R.|Yan, S.-J.|Lin, J.|
32	Palladium(II)-catalyzed cyclization of heterocyclic ketene aminals with (E)-ethyl 2,3-diiodoacrylates: selective synthesis of bicyclic pyrroles and bicyclic pyridones	期刊論文	Lin, Xin-Rong|Zhu, Hong-You|Yan, Sheng-Jiao|Lin, Jun|
33	Cascade reaction synthesis of multisubstituted bicyclic pyridone derivatives (vol 69, pg 9224, 2013)	期刊論文	Zhu, Dandan|Wang, Xiaoying|Yan, Shengjiao|Lin, Jun|

項目摘要

腫瘤是當今世界嚴重威脅人類生命與健康的疾病，成為死亡的頭號殺手。拓撲異構酶可通過催化DNA鏈的斷裂和結合控制其拓撲結構。拓撲異構酶 I成為公認的抗癌藥作用靶點。拓撲異構酶 I 抑制劑的研究開發有望解決目前臨床抗腫瘤藥物毒副作用及抗藥性等問題。茚並喹啉類化合物可有效抑制拓撲異構酶 I 從而表現出十分優越的抗腫瘤活性。本項目以茚並喹啉（6-Aryl-indeno[1,2-c]quinoline）為先導化合物設計合成茚並喹啉衍生物庫。並用雜環烯酮縮胺與吲哚醌一鍋法簡便合成80-100個目標化合物。擬對其進行抗腫瘤活性測試及構效關係研究。通過本項目的完成極有希望發現高效和高選擇性的抗腫瘤藥物或先導化合物。