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新型抗肿瘤药物研究是全球药物开发的重点任务之一。鉴于前期我们发现3,5-二取代1H-吲哚衍生物具有明显抗胰腺癌活性,本文通过维尔斯迈尔-哈克反应、仲胺的叔丁氧羰基(Boc)保护、醛还原、羧酸与胺的缩合等反应获得了一条高效简洁的3-取代硫甲基-5-酰氨基吲哚衍生物合成路线,并合成了8个新化合物11a~11h。经细胞活性测试发现,它们对胰腺癌细胞株BxPC-3均有较好抑制活性,其中11e活性最高,IC_(50)为2.28μmol/L。对多种肿瘤细胞及人正常肝细胞HL-7702的抑制活性测试表明,11e为特异性BxPC-3抑制剂而非细胞毒化合物。鉴于此,11e可能是一个较好的抗胰腺癌苗头化合物,值得进一步深入研究。 相似文献
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《有机化学》2016,(1)
首先合成吲哚醌衍生4a~4f,氧化水解得到邻氨基苯甲酸衍生物5a~5d.以这两者为原料设计合成A和/或D环取代的色胺酮衍生物1a~1q.然后,以色胺酮6位酮羰基分别与水合肼、盐酸羟胺反应生成C环席夫碱结构.最后,以哌嗪结构取代B环嘧啶酮合成茚(1,2-b)喹喔啉-11-酮.共设计合成20个化合物,其中新化合物13个.对所合成化合物的结构经红外光谱、核磁氢谱、元素分析确证.测定所合成化合物对肿瘤细胞A549的体外抑制活性.结果表明化合物1b,1c,1i,1j,1p和1q表现出较强的肿瘤细胞抑制活性,IC50值分别为3.58,0.99,1.03,2.10,0.51和0.43μmol·L-1.构效关系研究表明:D环卤素取代提高抗肿瘤活性,而取代基团在A环时则减弱抗肿瘤活性;B环(嘧啶环)被哌嗪环取代后抗肿瘤活性消失(IC50100μmol·L-1);而C环酮羰基生成席夫碱结构抗肿瘤活性与色胺酮相当. 相似文献
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《化学研究与应用》2020,(5)
以对硝基苯肼为起始原料,采用费舍尔吲哚合成法合成中间体5-硝基吲哚-2-羧酸酯(3),经还原合成5-氨基吲哚-2-羧酸酯(4),再与氯甲酸苯酯合成酰胺(5),5在水合肼作用下形成2,5-碳酰肼吲哚(6),化合物6和取代醛反应,合成了7个2,5-二取代吲哚碳酰肼衍生物(7a~7g)。目标化合物经~1HNMR、~(13)CNMR、HR-MS结构确证。采用MTT法研究了目标化合物的细胞毒活性。结果显示,目标化合物对所选肿瘤细胞的增殖活性具有一定抑制作用。其中7c对宫颈癌细胞(Hela)、乳腺癌细胞(MCF-7)和人肝癌细胞(HepG-2)的抑制活性与阳性药顺铂活性相近。 相似文献
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以取代苄氧基吲哚-3-甲醛和4-硝基苯肼为原料,乙醇为溶剂,通过缩合脱水反应合成了4个新化合物--取代苄氧基吲哚-3-甲醛-(4'-硝基)苯腙,其结构经1H NMR,IR,MS和元素分析表征. 相似文献
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基于双吲哚马来酰亚胺化合物和硫脲化合物的结构及多样的生物活性,通过1-氨基-3,4-二(吲哚-3-基)-3-吡咯啉-2,5-二酮与异硫氰酸酯反应,合成了17种新的3,4-二(吲哚-3-基)-2,5-二酮-1-吡咯亚胺硫脲类化合物,化合物的结构通过1H NMR、13C NMR、HRMS等进行了表征。该系列化合物的初步抗肿瘤活性测试表明,它们都对细胞周期分裂蛋白25B(CDC 25B)表现出良好的抑制活性(大部分化合物的抑制率在96%以上),具有潜在的抗肿瘤活性及应用价值。 相似文献
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以取代苄氧基吲哚-3-甲醛和4-硝基苯肼为原料,乙醇为溶剂,通过缩合脱水反应合成了4个新化合物——取代苄氧基吲哚-3-甲醛-(4′-硝基)苯腙,其结构经1H NMR,IR,MS和元素分析表征。 相似文献
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Synthesis and In Vitro Antitumor Evaluation of Some New Pyrimido[4,5‐b]quinoxaline 5,10‐Dioxide Derivatives 下载免费PDF全文
Mohamed Waly Sameh Elgogary Ahmed Lashien Ahmad Farag 《Journal of heterocyclic chemistry》2015,52(2):411-417
A new series of tricyclic pyrimidoquinoxaline derivatives were synthesized and evaluated as antitumor assays and compared with standard drug 5‐fluorouracil. These new pyrimidoquinoxaline derivatives were synthesized by the reaction with o‐aminonitrilequinoxaline derivative 3 with various reagents. One from which, the condensation of o‐aminonitrile with potassium cyanate in acetic acid was stated as a new procedure for building the pyrimidine ring incorporate to quinoxaline moiety. Further condensation of aminonitrile 3 with formamide or Vilsmeier reaction followed by transamination or carbon disulphide was applied as procedures for the pyrimidine ring syntheses. Compound 15 achieved significant in vitro antitumor activity, and compounds 9 and 14 have high activities. 相似文献
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Wafaa S. Hamama Alaa E. Hassanien Manal G. El‐Fedawy Hanafi H. Zoorob 《Journal of heterocyclic chemistry》2016,53(3):945-952
A series of α,β‐unsaturated ketones containing quinolone moieties 2 , 3 , 4 , 5 , 6 were synthesized by condensation of 7‐methoxyquinoline‐2,4(1H,3H)‐dione ( 1 ) with different aryl aldehydes. Pyrazole derivatives 8 , 9 , 10 , 11 were also synthesized via refluxing of α,β‐unsaturated ketones 2 , 3 , 4 , 5 , 6 with hydrazine derivatives. Newly synthesized compounds were characterized by elemental analyses, spectral data, and screened for their antioxidant and antitumor activities. Geometrical optimizations of the molecular structures for different synthesized compounds were studied. 相似文献
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Starting from 6-aryl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4a-d), a series of mono- and dialkyl derivatives 5a-j and 6a, b was synthesized. Hydrazinolysis of 4a, b, d and 5d afforded the hydrazino derivatives 7a-c which were cyclised to give the triazolopyrimidinones 8a-c and the pyrimidotriazinones 9a-c through the reaction with formic acid and chloroacetyl chloride, respectively. Most of the newly synthesized compounds were evaluated for their in-vitro antitumor activity. Compounds 6a and b displayed promising anticancer activity against leukaemia, non-small cell lung, melanoma, and renal cancer. On the other hand, all compounds prepared were screened for their in-vitro antibacterial and antifungal activities. Compounds 5h and j showed significant activity against Staphylococcus aureus, while compounds 5e, 7c and 8c displayed moderate inhibitory activity against Candida albicans. 相似文献
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以4,5-二甲氧基-2-氨基苯甲酸和醋酸甲眯为起始原料,经环化、氯化、取代和缩合四步反应,设计、合成了六个未见文献报道的含有缩氨基硫脲的喹唑啉衍生物4a~4f,其结构用1H NMR,13C NMR,ESI-MS,IR及元素分析测试技术进行了表征.采用MTT法测试了化合物4a~4f对人胃癌SGC-7901、人口腔表皮样癌KB和人纤维肉瘤HT-1080的体外抗肿瘤活性.初步的测试结果表明,化合物4a和4f对HT1080表现出显著的抗肿瘤活性. 相似文献
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合成了5个新的柔红霉素及阿霉素的氮氧自由基自旋标记衍生物(5_9),经元素分析,IR,MS和ESR分析确证了其组成和结构,并对它们进行了抑制小鼠白血病P388、小鼠黑色素癌B16、人胃腺癌MGC和人肝癌SMMC7721细胞的体外筛选.初步药理试验表明,化合物5_9对4种瘤株均有一定的抑制活性,其中化合物9的活性与阿霉素相当. 相似文献
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为了寻找高效低毒的抗肿瘤药物,设计并合成新型的1,3位取代酞嗪酮类化合物.采用噻唑蓝(MTT)法对目标化合物在MCF-7(人乳腺癌细胞)、PC-3(人前列腺癌细胞)、SW-620(人结肠癌细胞)和HGC-27(人胃癌细胞)四种人类癌细胞的抗增殖活性进行评价.结果显示大部分化合物具有较好的抗增殖活性.其中,2-(4-(4-溴苯基)-1-氧代酞嗪-2(1H)-基)-N-(2-氟苯基)乙酰胺(5g)对MCF-7细胞的抗增殖活性较好,IC50值为6.01μmol/L,为抗肿瘤药物的研究提供了思路. 相似文献
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Di Zao Li Yan Li Xiao Guang Chen Chen Gen Zhu Jing Yang Hong Yan Liu Xian Dao Pan 《中国化学快报》2007,18(11):1335-1338
A series of heterocyclic acid esters of camptothecins as new compounds had been synthesized by acylation method,their in vitro and in vivo antitumor activities were evaluated.The cytotoxic results showed that 6 possessed the best efficacy on six human cancer cell lines in the six classes of CPTs' derivatives.In vivo testing results indicated that 9 had better antitumor activity against mouse liver carcinoma H_(22) than topotecan. 相似文献
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Guanlin Zhong Jiayi Shen Zhengwang Chen Zunxian Lin Lipeng Long Jiaying Wu Chenhuan Long Siyu Huang Ping Lian Guotian Luo 《Molecules (Basel, Switzerland)》2022,27(3)
Hesperetin is a class of natural products with a wide range of sources and remarkable biological activities. In this study, we described the synthesis of a series of novel hesperetin derivatives and evaluated the in vitro antioxidant and antitumor activity of these compounds. Eleven novel compounds were synthesized in moderate yields. The compounds synthesized in this work exhibited antioxidant activities against DPPH and ABTS free radicals in a dose-dependent manner. Among them, compound 3f had the best antioxidant activity, with IC50 of 1.2 μM and 24 μM for DPPH and ABTS, respectively. The antitumor activity of the compounds against human cancer cell lines, such as breast MCF-7, liver HepG2, and cervical Hela, was determined by a standard 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. Three compounds had moderate IC50 values. Interestingly, compound 3f had better biological activity than hesperetin, which matches the prediction by Maestro from Schrödinger. Therefore, the new hesperidin derivative is a promising drug for the treatment of cancer due to its effective antitumor activity. The results also suggested that the antitumor activities of hesperetin derivatives may be related to their antioxidant activities. 相似文献
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Hala M. Aly 《Monatshefte für Chemie / Chemical Monthly》2011,20(7):935-941