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Zhen Yuan MIAO Wan Nian ZHANG Jian Zhong YAO Chun Quan SHENG Yun Long SONG Hui XU Min ZHANG Jing ZHANG 《中国化学快报》2006,17(6):720-722
Camptotecin is the parent of an important class of anticancer agents which, can selectively poison the ubiquitous nuclear enzyme topoisomerase. Water soluble camptothecin analogues such as topotecan and irinotecan are already approved for clinical uses in… 相似文献
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LIJuan WUXin-yu LIJing WANGHong-fang QIYan-fei YUXi-he SUNZhi-wei WANGEn-bo 《高等学校化学研究》2005,21(2):127-130
A novel 5-fluorouracil salt of 12-silicatungstic acid was synthesized and characterized by means of elemental analysis, IR,^1H NMR and ^183W NMR spectra. The antitumor activity and toxicity of the complex have been evaluated both in vitro and in vivo. 相似文献
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Guo Ping Wang Yue-Wu Luo Xin-Tong Qi Xiao-Lu Hou Le-Ping Xie Zi-Xin 《Phosphorus, sulfur, and silicon and the related elements》2013,188(4):511-518
Abstract γ-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted γ-aminopropylsilatrane derivatives were synthesized and assayed by a primary anticancer screening against HT-29, Hela, and MDAMB435 cells by the use of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The structures of these derivatives were confirmed by 1H NMR, electrospray ionization-mass spectrometry, and elemental analysis. The structure–activity relationship showed that the N-substituted derivatives exhibit better activity in which the γ-amino group of the silatrane is connected with stronger electron-withdrawing groups. 相似文献
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Volkov V. A. Voronkov M. V. Sazhina N. N. Kurilov D. V. Vokhmyanina D. V. Yamskova O. V. Martirosyan Yu. Ts. Atroshenko D. L. Martirosyan L. Yu. Romanova V. S. 《Kinetics and Catalysis》2021,62(3):395-403
Kinetics and Catalysis - The kinetic characteristics, mechanisms of activity, and relationship between the antioxidant activity and the molecular and supramolecular structure of fullerene C60 and... 相似文献
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8, 8-Dimethyl-5, 6, 7,8-tetrahydrophenanthrene-3, 4-dione (3) and 8, 8-dimethyl-2- ( 1-hydroxy ethyl) -5,6, 7, 8-tetrahydrophenanthrene-3,4-dione (4), two analogues of the antitumor active tanshinone, were synthesized from anisole. The synthesized compounds 3 and 4 were shown to be highly active against leukemia P-388 cell fine as assayed by in vitro MTT method. 相似文献
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Mala Nath Hitendra Singh George Eng Xueqing Song 《Phosphorus, sulfur, and silicon and the related elements》2013,188(6):755-767
Abstract New triorganotin(IV) derivatives of dipeptides with general formulae, R3Sn(HL), where R = Me and Ph, and HL is the monoanion of histidinylalanine and histidinylleucine, have been synthesized and characterized on the basis of infrared (IR), multinuclear NMR (1H, 13C, and 119Sn), and 119Sn Mössbauer spectroscopic studies. These derivatives exhibit distorted trigonal-bipyramidal geometry around tin in which dipeptide anion acts as bidentate ligand coordinating through carboxyl oxygen and amino nitrogen. Ph3Sn(HHis-Ala), Ph3Sn(HHis-Leu), and previously reported Ph2Sn(His-Ala), Me2Sn(His-Ala), n-Oct2Sn(His-Ala), Me2Sn(His-Leu), n-Oct2Sn(His-Leu), Ph3Sn(HTyr-Phe), Ph2Sn(Tyr-Phe), Bu2Sn-(Tyr-Phe), and n-Oct2Sn(Tyr-Phe) along with standard drugs, viz. phenyl butazone and indomethacin were screened for in vivo anti-inflammatory activity and acute toxicity (LD50). Diorganotin(IV) derivatives are more active than triorganotin(IV) derivatives. Me2Sn(His-Leu) shows the highest activity. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
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Ye WANG Yan Li ZHOU Zhan Zhu LIU Shi Zhi CHEN Xiao Guang CHEN 《中国化学快报》2006,17(10):1279-1282
Ecteinascidin 743 (Et-743) is an exceedingly potent antitumor agent isolated from the extracts of the marine tunicate Ecteinascidia turbinate1 that is currently undergoing phase Ⅱ/Ⅲ clinical trials in Europe and the United States2. As the result of its … 相似文献
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《合成化学》2004,(Z1)
Isosteviol (ent-16-ketobeyeran-19-oic acid, I) is a tetracyclic diterpenoid with a beyerane skeleton obtained by acid hydrolysis of stevioside.1 Several tetracyclic diterpenoids, specially the kaurenes, have important biological activities. Recent studies on the microbial transformation of isosteviol have revealed that it is metabolized by Cunninghamella bainieri, Actinoplanes sp., Mucor recurvatus, and Cunninghamella blackesleeana to yield five new metabolites.2 The hydroxylation pattern of… 相似文献
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Synthesis and Structure Elucidation of Celangulin Derivatives 总被引:1,自引:0,他引:1
Celangulins are sesquiterpene polyol esters based on a core structure known as β-dihydroagarofuran from Celastrus angulatus Max. Some of them are environment acceptable-pesticides. In order to find new active compounds and study their SAR, sesquiterpene polyol esters libraries were synthesized based on the basic hydrolysis of the extract of the root bark of Celastrus angulatus which could offer the β-dihydroagarofuran polyol by combinatorial chemical method and the compounds with insecticidal activity were isolated by bioassay-guided fractionation. Two new compounds with insecticidal activity against Mythimna separata, were isolated and elucidated as 2β,6α,8β, 13-tetraisobutanoyloxy-1β,4,9α-trihydroxy-β-dihydroagarofuran (A) and 1β,2β,6α,8β, 13-pentaisobutanoyloxy-4α,9α-dihydroxy-β-dihydroagarofuran (B) mainly by 1H NMR, 13C NMRH-HCOSY, HMQC, HMBC and HRMS spectral data. A: [α]20D -7.3 (c 0.12, CHCl3), B: [α]20D -34.6 (c 0.8,CHCl3). 相似文献
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A series of 1-glycosyl-2-glycosylthiopyrimidine (4), annelated pyrimidine derivatives, pyrazolo[3,4-d]-pyrimidine (8), ditetrazolo[1,5-a;1‘,5‘-c]pyrimidine (9), 2,9a,10-triazaanthracene (12), thieno[2,3-d]pyrimidine (14),9-thia-1,3,5,7-tetraazafluorene-8-one (15), 7-oxa-9-thia-1,3,5-triazafluorene-8-one (16), 5-oxa-9-thia-1,3-diaza-fluorene (21a and 21b) derivatives have been synthesized via a sequence of heterocyclization reactions of suitably functionalized 6-[5-(4-bromophenyl)oxazol-4-yl]-1,2,3,4-tetrahydro-2-thioxo-4-oxopyrimidine-5-carbonitrile (2) with different electrophiles and nucleophiles. The new compounds were prepared with the objective to study their pharmacological properties. 相似文献
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Classical antifolates containing L-glutamic acid moiety in molecule have shortcomings such as drug resistance which is originated from the defective cell transport by mutation, and toxicity to the host which is due to unnecessarily long retention inside normal cells.[1] One strategy to overcome these shortcomings is to design nonclassical lipophilic inhibitors of folate requiring enzymes by deleting or modifying L-glutamic acid component from the folate analogues. 相似文献
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y-Aminobutyricacidisregardedasoneofthemaj0rinhibit0ryneur0transmittersinthemammaliancentralnervoussystem."'UnderPhysiologicalconditi0ns,y-aminobutyricacidpo0riycrossestheb1ood-brainbarrier.SoitisnoteffectivebyoraladministTation.3'4ItisIikelythatan0n-toxicderivativeofy-arninobutyricacidwhichentersthebraineasilywi1lhaveusefultheraPeuticproperties.Withthisinmind,wehavedesignedandsynthesizedl6derivativesofy-aminobubocacidwithaniminelinktoa1ip0philiccarrierinordert0facilitatethepassage0fy-aminobu… 相似文献
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Kumar K. Santhosh Siddaiah V. Lilakar J. D. Sunanda K. Ganesh A. 《Russian Journal of Organic Chemistry》2020,56(11):2014-2021
Russian Journal of Organic Chemistry - An efficient and simple continuous-flow synthetic protocol for novel quinoline-tethered pyrazoline derivatives, which involves condensation of... 相似文献
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ChunQuanSHENG WanNianZHANG HaiTaoJI YunLongSONG 《中国化学快报》2004,15(4):404-407
Twenty-one 1-(1H-1,2,4-triazolyl)-2-(2,4-diflurophenyl)-3-(4-substituted-1-piperazinyl)-2-propanol derivatives were designed and synthesized,on the basis of the active site of lanosterol 14α-demethylase.In vitro antifungal activities showed that some of the target compounds had higher antifungal activity and broader antifungal spectrum than fluconazole. 相似文献
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YanFangZHAO JinHuaDONG PingGONG 《中国化学快报》2004,15(9):1039-1042
A series of ethyl 6-bromo-5-hydroxyindole-3-carboxylate derivatives were synthesized and their in vitro anti-influenza virus activity was evaluated. All the compounds were characterized by ^1H NMR and MS. 相似文献
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Synthesis of Hydroxystilbene Derivatives and their Antioxidant Activity by DPPH Method 总被引:5,自引:0,他引:5
IntroductionThe increasing interest in the research on antioxi-dants is attributed to the availability of vastevidence re-garding the importance of reactive oxygen/nitrogen spe-cies(ROS/RON) in the processes of aging and patho-genesis. It has been suggest… 相似文献
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5-Fluorouracil (5-Fu,1)1 is an important antitumor drug. Some derivatives2,3 have shown better therapeutic efficacy than 5-Fu. In order to find much more better antitumor drugs of its derivatives, several attempts have been made and many different types of its derivatives have been prepared at N1, N3 position4~7. Moreover, several different ways have been used for alkylation of 5-Fu7~10. However, up to now, the arylation of 5-Fu at N1 or N3 position hasn't been reported, and the compound o… 相似文献