- Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents
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Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their in?vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50 values of 25?682?nm against various types of cancer cell l
- Cao, Dong,Wang, Xiaoyan,Lei, Lei,Ma, Liang,Yang, Zhuang,Wang, Fang,Chen, Lijuan
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- Quinazoline derivative and preparation method and application thereof
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The invention discloses a novel compound 4-(3 '-R substituted-5'-R substituted-4 '-hydroxyanilino) quinazoline derivative and a preparation method and application thereof. The structural formulas of the compound are shown as formulas I and II. The compound has good activity of preventing and treating chicken coccidiosis and can be used as a therapeutic agent for preventing and treating chicken coccidiosis in the field of preparation of medicines for preventing and treating chicken coccidiosis.
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Paragraph 0039-0041; 0046-0047; 0050-0051; 0054-0055; 0058
(2020/07/15)
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- Synthesis and biological evaluation of quinazoline derivatives – A SAR study of novel inhibitors of ABCG2
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Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of cancer frequently leading to failure of the therapy. MDR is often associated with the overexpression of ABC transport proteins like ABCB1 or ABCG2 which efflux harmful substances out of cells at the cost of ATP hydrolysis. One way to overcome MDR is to apply potent inhibitors of ABC transporters to restore the sensitivity of the cells toward cytostatic agents. This study focusses on the synthesis and evaluation of novel 2,4-disubstituted quinazoline derivatives regarding the structure-activity-relationship (SAR), their ability to reverse MDR and their mode of interaction with ABCG2. Hence, the inhibitory potency and selectivity toward ABCG2 was determined. Moreover, the intrinsic cytotoxicity and the reversal of MDR were investigated. Interaction type studies with the substrate Hoechst 33342 and conformational analyses of ABCG2 with 5D3 monoclonal antibody were performed for a better understanding of the underlying mechanisms. In our study we could further enhance the inhibitory effect against ABCG2 (compound 31, IC50: 55 nM) and identify the structural features that are crucial for inhibitory potency, the impact on transport activity and binding to the protein.
- Krapf, Michael K.,Gallus, Jennifer,Spindler, Anna,Wiese, Michael
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p. 506 - 525
(2018/11/06)
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- A novel strategy to the synthesis of 4-anilinoquinazoline derivatives
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A novel approach to prepare 4-anilinoquinazoline derivatives based on the transformation of indoline-2,3-dione to formamidine was developed. The processes with this approach are simple, efficient, and environmentally friendly. The efficiency of this approach was evaluated by synthesizing 17 4-anilinoquinazolines and comparing the obtained yields with those achievable through conventional synthetic methods. It was the first time that compounds 8d, 8e, 8h, and 13b-f were synthesized. The characteristics of the IR and the UV spectra of these compounds and the effects of their substituents on the spectra were observed.
- Wang, Zheng,Wang, Cuiling,Sun, Yanni,Zhang, Ning,Liu, Zhulan,Liu, Jianli
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p. 906 - 913
(2014/01/23)
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- Phthalazine compounds, compositions and use
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The present invention relates to new compounds of the formula STR1 alkylene, or --S-- where R1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y)A is --CH2 NR2/s
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- Studies in Potential Filaricides: Part XI - Synthesis of 2-Dialkylaminomethyl-4-substitutedamino-phenols as Amodiaquine Analogs
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A number of 4,7-disubstituted quinazolines (11-17) and 2-dialkylaminomethyl-4-acetylaminophenols (19-30) have been synthesized and tested for their antifilarial activity against Litosomoides carinii in cotton rat (Sigmodon hispidus).Of the compounds tested 19-21 and 26 cause 60percent fall in microfilarial count at a dose of 30 mg/kg given intraperitoneally daily for 6 days.None of the compounds possesses any macrofilaricidal activity.
- Agrawal, V. K.,Sharma, Satyavan,Iyer, R. N.,Chatterjee, R. K.,Sen, A. B.
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p. 1084 - 1087
(2007/10/02)
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