521-74-4Relevant articles and documents
Synthesis, cytotoxicity and structure-activity relationship of indolizinoquinolinedione derivatives as DNA topoisomerase IB catalytic inhibitors
Yu, Qian,Yang, Hui,Zhu, Teng-Wei,Yu, Le-Mao,Chen, Jian-Wen,Gu, Lian-Quan,Huang, Zhi-Shu,An, Lin-Kun
, p. 195 - 207 (2018)
Our previous studies reveal that indolizinoquinolinedione scaffold is a base to develop novel DNA topoisomerase IB (TOP1) catalytic inhibitors. In this work, twenty-three novel indolizinoquinolinedione derivatives were synthesized. TOP1-mediated relaxation, nicking and unwinding assays revealed that three fluorinated derivatives 26, 28 and 29, and one N,N-trans derivative 46 act as TOP1 catalytic inhibitors with higher TOP1 inhibition (++++) than camptothecin (+++) and without TOP1-mediated unwinding effect. MTT assay against five human cancer cell lines indicated that the highest cytotoxicity is 20 for CCRF-CEM cells, 25 for A549 and DU-145 cells, 26 for HCT116 cells, and 33 for Huh7 cells with GI50 values at nanomolar range. The drug-resistant cell assay indicated that compound 26 may mainly act to TOP1 in cells and are less of Pgp substrates. Flow cytometric analysis showed that compounds 26, 28 and 29 can obviously induce apoptosis of HCT116 cells. Moreover, the structure-activity relationship (SAR) of indolizinoquinolinedione derivatives was analyzed.
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Ito
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Tricycloisoxazole compound and preparation and application methods thereof
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Paragraph 0207-0208, (2019/03/31)
The invention discloses a tricycloisoxazole compound and a medically acceptable salt thereof. The structure of the tricycloisoxazole compound is shown as the formula I, wherein A is thienyl, furyl, phenyl and pyridyl; R1 is hydrogen, halogen, amido, substituted amido, nitro, acylamino, substituted acylamino, cyan, low alkyl and alkoxy; R2 is alkyl, alkoxy, alkoxy alkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heterocyclyl; R3 is carbon or hydroxyl; X is carbon atom or oxygen atom, and when being carbon atom, is connected with the substituted group R3, which is carbonyl or carboxyl. The invention also provides preparation and application methods of the tricycloisoxazole compound, namely, the tricycloisoxazole compound can serve as an antifungal small-molecule inhibitor. In vitro antifungal activity experiment results show that most of the tricycloisoxazole compound shown as the formula I achieves good antifungal activity, especially significantly higher antifungal activity on Cryptococcus neoformans compared with a positive fungicide of fluconazole, thereby being applicable to preparing antifungal drugs.
Study on Relationship Between Fluorescence Properties and Structure of Substituted 8-Hydroxyquinoline Zinc Complexes
Jianbo, He,Tingting, Zhou,Yongjing, Cao,Yuanyuan, Zhang,Weiqing, Yang,Menglin, Ma
, p. 1121 - 1126 (2018/08/17)
Organic light-emitting diodes (OLEDs) produced from 8-hydroxyquinoline metal complexes play a vital role in modern electroluminescent devices. In this manuscript, a series of 8-hydroxyquinoline derivatives were synthesized by different methods and their corresponding zinc metal complexes were prepared. The UV and fluorescence properties of the complexes were measured aiming to understand the effect of substituents at the quinoline ring on the fluorescence properties of the complexes. When the C-5 of 8-hydroxyquinoline was replaced by halogen group, the fluorescence emission wavelengths had been red-shifted, at the same time, blue-shifted of fluorescence emission wavelength was observed when the C-5 position of 8-hydroxyquinoline was substituted by electron-withdrawing group. When the C-4 position of 8-hydroxyquinolie was substituted by methyl or the C-5 position was substituted by sulfonic acid group, the corresponding zinc complexes had higher fluorescence intensity than 8-hydroxyquinolie zinc.
