Synthesis and cytotoxicity of O,O′-dialkyl {[2-(substituted phenoxy)acetamido](substituted phenyl)methyl}phosphonates
作者:
Ning, Lihong;Wang, Wei;Liang, Yongju;Peng, Hao;Fu, Liwu* ;...
期刊:
European Journal of Medicinal Chemistry ,2012年48:379-384 ISSN:0223-5234
通讯作者:
Fu, Liwu
作者机构:
[He, Hongwu; Peng, Hao; Wang, Wei; Ning, Lihong] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;[Liang, Yongju; Fu, Liwu] Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.;[He, Hongwu; Peng, Hao; Wang, Wei; Ning, Lihong] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Fu, Liwu] S;Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.
关键词:
Synthesis;Cytotoxicity;Phosphonate
摘要:
A series of O,O′-dialkyl {[2-(substituted phenoxy)acetamido] (substituted phenyl)methyl}phosphonates was synthesized and their cytotoxic activities were tested against various human tumor cell lines. Some compounds (5q, 5r, 5s, 5w, 5x and 5y) showed relatively high cytotoxicity. Especially, compounds 5x and 5q exhibited the best cytotoxicity against KB and CNE2 cells with IC 50 7.1 and 11.4 μM, respectively. Their inhibitory activities against KB and CNE2 cells were even higher than that of fluorouracil. © 2011 Elsevier Ltd. All rights reserved.
语种:
英文
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SYNTHESIS, CHARACTERIZATION, AND FUNGICIDAL ACTIVITY OF NEW THIENOPYRIDOPYRIMIDINE DERIVATIVES
作者:
Liu, Jian-Chao;He, Hong-Wu*
期刊:
Synthetic Communications ,2012年42(14):2075-2082 ISSN:0039-7911
通讯作者:
He, Hong-Wu
作者机构:
[He, Hong-Wu; Liu, Jian-Chao] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hong-Wu] C;Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
关键词:
Aza-Wittig reaction;carbodiimide;fungicidal activity;iminophosphorane;pyrido[4,3-d[pyrimidin-4(3 H)-ones
摘要:
Iminophosphorane 3 is a important intermediate in organic synthesis. A series of new 2-substituted tetrahydrobenzo[4′,5′]thieno[3′, 2′:5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones 5 have been designed and synthesized via the tandem aza-Wittig reaction in 58-92% yields. Iminophosphorane 3 reacted with phenyl isocyanate (or 4-chlorophenyl isocyanate, 4-fluorophenyl isocyanate) to give carbodiimide 4, which was further treated with amines to cyclize in the presence of a catalytic amount of EtONa. The structures of compounds 5 have been confirmed by 1H NMR, electron-impact mass spectrometry, infrared spectroscopy, and elemental analyses. The results of preliminary bioassay indicated that some compounds possess inhibition activities against Rhizoctonia solani and Botrytis cinereapers at a dosage of 50mg/L. © 2012 Taylor & Francis Group, LLC.
语种:
英文
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2-[(4-Chlorophenyl)(hydroxy)meth-yl]-5,5-dimethyl-1,3,2-dioxaphosphinan-2- one
作者:
Wang, Chubei;Peng, Hao;He, Hongwu*
期刊:
Acta Crystallographica Section E: Crystallographic Communications ,2011年67(4):O926-U977 ISSN:2056-9890
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Peng, Hao; Wang, Chubei] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Coll Chem, Wuhan 430079, Peoples R China.
摘要:
In the title compound, C12H16ClO4P, the phospho-nate ring adopts a chair conformation. In the crystal, intermolecular O - H⋯O hydrogen bonds link the molecules into chains propagating along the b axis.
语种:
英文
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无卤阻燃剂研究进展
作者:
张翔宇;黄琰;游歌云;贺红武
期刊:
精细化工中间体 ,2011年41(3):1-8 ISSN:1009-9212
作者机构:
华中师范大学农药与化学生物学重点实验室化学学院有机合成研究所,湖北武汉,430079;[贺红武; 张翔宇; 游歌云; 黄琰] 华中师范大学
关键词:
无卤阻燃剂;阻燃技术;研究进展
摘要:
综述了近年来国内外无卤阻燃剂的种类及研究进展,包括无机阻燃剂、有机磷系、有机硅系、氮系以及膨胀型阻燃剂。并对今后阻燃技术发展趋势进行了展望。
语种:
中文
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Studies of O,O-Dimethyl alpha-(2,4-Dichlorophenoxyacetoxy)ethylphosphonate (HW02) as a New Herbicide. 1. Synthesis and Herbicidal Activity of HW02 and Analogues as Novel Inhibitors of Pyruvate Dehydrogenase Complex
作者:
He, Hong-Wu* ;Yuan, Jun-Lin;Peng, Hao;Chen, Ting;Shen, Ping;...
期刊:
Journal of Agricultural and Food Chemistry ,2011年59(9):4801-4813 ISSN:0021-8561
通讯作者:
He, Hong-Wu
作者机构:
[Tan, Hong-Liang; Peng, Hao; He, Jun-Bo; He, Hong-Wu; He, Ya-Hui; Li, Yan; Chen, Ting; Li, Yanjun; Shen, Ping; Wan, Shu-Qing; Yuan, Jun-Lin] Cent China Normal Univ, Coll Chem, Inst Pesticide Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hong-Wu] C;Cent China Normal Univ, Coll Chem, Inst Pesticide Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.
关键词:
alpha-(substituted phenoxyacetoxy)alkylphosphonate;herbicidal activity;pyruvate dehydrogenase complex;inhibitor;structure-activity relationships
摘要:
On the basis of the previous work for optimization of O,O-diethyl α-(substituted phenoxyacetoxy)alkylphosphonates, further extensive syntheticmodifications were made to the substituents in alkylphosphonate and phenoxymoieties of the title compounds. New O,O-dimethyl α-(substituted phenoxyacetoxy)alkylphosphonates were synthesized as potential inhibitors of pyruvate dehydorogenase complex (PDHc). Their herbicidal activity and efficacy in vitro against PDHc were examined. Some of these compounds exhibited significant herbicidal activity and were demonstrated to be effective inhibitors of PDHc from three different plants. The structure-activity relationships of these compounds including previously reported analogous compoundswere studied by examining their herbicidal activities. Both inhibitory potency against PDHc and herbicidal activity of title compounds could be increased greatly by optimizing substituent groups of the title compounds. O,O-Dimethyl α-(2,4- dichlorophenoxyacetoxy)ethylphosphonate (I-5), which acted as a competitive inhibitor of PDHc with much higher inhibitory potency against PDHc from Pisum sativum and Phaseolus radiatus than from Oryza sativa, was found to be themost effective compound against broadleaf weeds and showed potential utility as herbicide. ©2011 American Chemical Society.
语种:
英文
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A Facile Synthesis of Novel Thiazolo[4,5-d]pyrimidin-7-ones
作者:
Liang, Ying* ;He, Hong-Wu;Yang, Zi-Wen
期刊:
Journal of Heterocyclic Chemistry ,2011年48(1):88-91 ISSN:0022-152X
通讯作者:
Liang, Ying
作者机构:
[Yang, Zi-Wen; Liang, Ying] Hubei Acad Agr Sci, Lab Green Chem & Synth, Hubei Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China.;[He, Hong-Wu; Liang, Ying] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Liang, Ying] H;Hubei Acad Agr Sci, Lab Green Chem & Synth, Hubei Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China.
摘要:
Sixteen 5‐alkylamino‐3,6‐diaryl‐2‐thioxo‐2,3,6,7‐tetrahydrothiazolo[4,5‐d]pyrimidin‐7‐ones 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j, 4k, 4l, 4m, 4n, 4o, 4p were designed and easily synthesized via a tandem aza‐Wittig reaction. The iminophosphorane 2, obtained from reaction of 1 with triphenylphosphine, hexachloroethane and Et3N, reacted with aromatic isocyanate to give carbodiimide 3. carbodiimide 3 reacted with alkylamines to provide the title compounds in 45–61% isolated yields in presence of catalytic amount of ethoxide. The structures of compounds 4 were confirmed by 1H NMR, IR, MS, and elemental analysis. J. Heterocyclic Chem., 2011.
语种:
英文
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Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas
作者:
Peng, Hao;Liang, Yongju;Chen, Le;Fu, Liwu* ;Wang, Haiqin;...
期刊:
Bioorganic & Medicinal Chemistry Letters ,2011年21(4):1102-1104 ISSN:0960-894X
通讯作者:
Fu, Liwu
作者机构:
[He, Hongwu; Peng, Hao; Wang, Haiqin; Chen, Le] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;[Liang, Yongju; Fu, Liwu] Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.;[He, Hongwu; Peng, Hao; Wang, Haiqin; Chen, Le] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Fu, Liwu] S;Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.
关键词:
1,3-Benzenedicarbonyl dithioureas;Antitumor activity;Synthesis
摘要:
The synthesis and biological activity of 1,3-benzenedicarbonyl dithioureas are described. Bioassay results indicated that these compounds exhibited cytotoxicity against various cancer cells. For example, compounds 4a showed the best inhibition activities against KB and CNE2 with IC50 10.72 and 9.91 μM, respectively. © 2010 Elsevier Ltd. All rights reserved.
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英文
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(S)-2-[1-(4-Bromo-phen-yl)-1-hy-droxy-ethyl]-5,5-dimethyl-1,3, 2-dioxaphos-phinane 2-oxide
作者:
Wang, Chubei;Peng, Hao;He, Hongwu*
期刊:
Acta Crystallographica Section E: Crystallographic Communications ,2011年67(7):O1739-U1156 ISSN:2056-9890
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Peng, Hao; Wang, Chubei] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Coll Chem, Wuhan 430079, Peoples R China.
摘要:
In the crystal structure of the title mol-ecule, C 13H 18BrO 4P, the phospho-nate ring adopts a chair conformation. Mol-ecules are linked by an O - H⋯O hydrogen bond [O⋯O = 2.780 (3) Å] to form chains parallel to the c axis. Two C - H⋯O inter-actions help to stabilize the crystal structure. © Wang et al. 2011.
语种:
英文
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2-氨基(芳氧基)-3-对甲基苯基噻吩并[3’,2’:5,6]吡啶并[4,3-d]嘧啶-4(3H)-酮的合成和生物活性
作者:
Liu Jianchao* ;He Hongwu;Chen Helian
期刊:
有机化学 ,2011年31(8):1208-1212 ISSN:0253-2786
通讯作者:
Liu Jianchao
作者机构:
[Chen Helian; Liu Jianchao; He Hongwu] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Liu Jianchao] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Coll Chem, Wuhan 430079, Peoples R China.
关键词:
乙酰乙酸甲酯;Aza-Wittig法;噻吩并吡啶;吡啶并嘧啶;杀菌活性
摘要:
用邻氨基噻吩腈与乙酰乙酸甲酯为原料,利用串联Aza-Wittig法合成了9个未见文献报道的噻吩并吡啶并嘧啶类化合物,通过IR,1H NMR,EI-MS,元素分析等方法对所合成的化合物进行了结构表征,并初步测定了所合成化合物的杀菌活性.生测结果表明:此类化合物对棉花枯萎(Fusarium oxysporium)、水稻纹枯(Rhizoctonia solani)、小麦赤霉(Gibberella zeae)、苹果轮纹菌(Dothiorella gregaria)、棉花炭疽菌(Colletotrichum gossypii)等5种菌均有一定的抑制活性.其中对苹果轮纹菌抑制活性最好,在浓度为5.0×10-5 g/mL时抑制率为31.80%~82.84%.
语种:
中文
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Structure-based rational design of novel hit compounds for pyruvate dehydrogenase multienzyme complex E1 components from Escherichia coli
作者:
Ren, Yanliang;He, Junbo;Feng, Lingling;Liao, Xun;Jin, Jing;...
期刊:
Bioorganic & Medicinal Chemistry ,2011年19(24):7501-7506 ISSN:0968-0896
通讯作者:
Wan, Jian
作者机构:
[He, Hongwu; He, Junbo; Jin, Jing; Wan, Jian; Li, Yongjian; Ren, Yanliang; Liao, Xun; Cao, Yi; Feng, Lingling] Cent China Normal Univ, Dept Chem, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Wan, Jian] C;Cent China Normal Univ, Dept Chem, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
Pyruvate dehydrogenase;Structure-based molecular docking;Molecular dynamics simulation;Fragment molecular orbital
摘要:
Pyruvate dehydrogenase multienzyme complex (PDHc) E1 component plays a pivotal role in cellular metabolism to convert the product of glycolysis (pyruvate) to acetyl-CoA, and has been reported as a potential target for anti-microbial and herbicide. In present study, based on the thiamin diphosphate (ThDP) site, four novel hit compounds with high inhibitory activity against the PDHc-E1 from Escherichia coli were firstly designed by using structure-based molecular docking methods. As expected, among four compounds, the compound 3a is the best inhibitor by far, with IC 50 value of 6.88 μM against PDHc-E1 from E. coli. To elucidate the interaction mechanism between the active site of PDHc-E1 and its inhibitor, the docking-based molecular dynamics simulation (MD) and MD-based ab initio fragment molecular orbital (FMO) calculations were also further performed. The positive results indicated that all modeling strategies presented in the current study most like to be an encouraging way in design of novel lead compounds with structural diversity for PDHc-E1 in the future. © 2011 Elsevier Ltd. All rights reserved.
语种:
英文
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Two Unusual Xanthones from the Bark of Garcinia xanthochymus
作者:
Chen, Yu;Fan, Hua;Yang, Guang-Zhong* ;Jiang, Yan;Zhong, Fang-Fang;...
期刊:
Helvetica Chimica Acta ,2011年94(4):662-668 ISSN:0018-019X
通讯作者:
Yang, Guang-Zhong
作者机构:
[He, Hong-Wu; Yang, Guang-Zhong; Chen, Yu] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;[He, Hong-Wu; Yang, Guang-Zhong; Chen, Yu] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China.;[Chen, Yu] S Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.;[Fan, Hua; Zhong, Fang-Fang; Yang, Guang-Zhong; Jiang, Yan] S Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, Wuhan 430074, Peoples R China.
通讯机构:
[Yang, Guang-Zhong] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
Antioxidant activity;Garcinia xanthochymus;Xanthones
摘要:
A new xanthone derivative, garcinexanthone F (1), which was found to possess an α,β-unsaturated γ-lactone moiety, and a new bisxanthone, bigarcinenone B (2), with a terpene bridge providing the xanthone-xanthone linkage, were isolated from the bark of Garcinia xanthochymus. Their structures were elucidated by spectroscopic methods, especially 2D-NMR techniques. The antioxidant assay in vitro showed that compounds 1 and 2 exhibited significant scavenging activities against 1,1-diphenyl-2- picrylhydrazyl (DPPH) radical with IC50 values of 22.32 and 20.14 μM, and against HO. radical with IC50 values of 1.16 and 2.85 μM, respectively. Copyright © 2011 Verlag Helvetica Chimica Acta AG, Zürich, Switzerland.
语种:
英文
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Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines
作者:
Mo, Wen-Yan;Liang, Yong-Ju;Gu, Yu-Cheng;Fu, Li-Wu* ;He, Hong-Wu
期刊:
Bioorganic & Medicinal Chemistry Letters ,2011年21(19):5975-5977 ISSN:0960-894X
通讯作者:
Fu, Li-Wu
作者机构:
[Mo, Wen-Yan; He, Hong-Wu; Gu, Yu-Cheng] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Sch Chem, Wuhan 430079, Peoples R China.;[Fu, Li-Wu; Liang, Yong-Ju] Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.;[Gu, Yu-Cheng] Syngenta, Jealotts Hill Int Res Ctr, Bracknell RG42 6EY, Berks, England.
通讯机构:
[Fu, Li-Wu] S;Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.
关键词:
Antitumor activity;MTT;Pyrido[4,3-d]pyrimidine;Synthesis
摘要:
Synthesis and cytotoxicity of 11 4-methylene pyrido[4,3-d]pyrimidines 5a-k were described. Cytotoxicity assay results showed that some compounds had much stronger antitumor activity than Fluorouracil against KB cell lines. The most active compound 5i exhibited high potency against KB, CNE2, MGC-803 cell lines with IC 50 values of 0.48, 0.15, 0.59 μM, respectively. The preliminary structure-activity relationships indicated that the introduction of benzyl groups bearing electron-donating function groups is favorable for the activity. © 2011 Elsevier Ltd. All rights reserved.
语种:
英文
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SYNTHESIS AND HERBICIDAL ACTIVITY OF NOVEL DIALKOXYPHOSPHORYL ARYL METHYL 2-(4,6-DIMETHOXYPYRIMIDIN-2-YLOXY) BENZOATE DERIVATIVES
作者:
Jin, Chuanfei;He, Hongwu*
期刊:
Phosphorus, Sulfur, and Silicon and the Related Elements ,2011年186(7):1397-1403 ISSN:1042-6507
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Jin, Chuanfei] Cent China Normal Univ, Inst Pesticide Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Inst Pesticide Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
Herbicidal activity;phosphonate;pyrimidinyl benzoate
摘要:
A series of dialkoxyphosphoryl aryl methyl 2-(4,6-dimethoxy-pyrimidin-2- yloxy) benzoate derivatives was designed and synthesized. All new compounds were identified by elemental analysis, infrared (IR), 1H-NMR, and mass spectrometry (MS). Their herbicidal activity against a set of weed species was examined. Some of the compounds showed potential herbicidal activity, which provided some indications for further studies on structure modification. 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. © 2011 Taylor & Francis Group, LLC.
语种:
英文
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有机协效阻燃剂的研究与应用
作者:
张宏;蔡哲;张翔宇;贺红武
期刊:
材料导报 ,2011年(1):457-463 ISSN:1005-023X
作者机构:
华中师范大学农药与化学生物学重点实验室化学学院有机合成研究所
关键词:
阻燃剂;协同效应;高分子材料
摘要:
阻燃剂的协同效应理论是提高高分子材料阻燃效率的一种有效手段,已成为当前研究开发高效阻燃剂的主要、指导理论之一。其中,围绕磷开展的高效有机协效阻燃剂研究开发是当前阻燃剂开发领域的热点。重点介绍了近10年来国内外研发的新型磷-卤素、磷-氮和磷-硅有机协效阻燃剂的研究进展,展望了阻燃剂未来的发展方向和前景。
语种:
中文
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Synthesis and antitumor activity of ureas containing pyrimidinyl group
作者:
Jin, Chuanfei;Liang, Yong-Ju;He, Hongwu* ;Fu, Liwu
期刊:
European Journal of Medicinal Chemistry ,2011年46(1):429-432 ISSN:0223-5234
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Jin, Chuanfei] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;[Liang, Yong-Ju; Fu, Liwu] Sun Yat Sen Univ, Ctr Canc, State Key Lab Oncol S China, Guangzhou 510060, Guangdong, Peoples R China.;[He, Hongwu] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, 152 Luoyu Rd, Wuhan 430079, Peoples R China.
关键词:
Urea;4,6-Dimethy-2-(methylsulfonyl)pyrimidine;Cytotoxicity
摘要:
A novel series of ureas containing pyrimidinyl group were designed and synthesized. Some of the prepared compounds showed potential cytotoxicity against several human cancer cell lines. From the structure-activity relationships we may conclude that introduction of a sulfide bridge between phenyl and pyrimidinyl rings would be critical for their biological activities.
语种:
英文
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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PHOSPHONATES DERIVATIVES OF AS POTENTIAL ANTITUMOR AGENTS
作者:
Jin, Chuanfei;Liang, Yong-Ju;He, Hongwu* ;Fu, Liwu
期刊:
Phosphorus, Sulfur, and Silicon and the Related Elements ,2011年186(10):2096-2103 ISSN:1042-6507
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Jin, Chuanfei] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Liang, Yong-Ju; Fu, Liwu] Sun Yat Sen Univ, Ctr Canc, State Key Lab Oncol S China, Guangzhou 510275, Guangdong, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
Phosphonate;amide;antitumor activity;pyrimidinylbenzoate
摘要:
Abstract A series of dialkyl [2-(4,6-dimethoxypyrimidin-2-yloxy)benzamido](aryl) methylphosphonates derivatives were designed and synthesized. All the new compounds were identified by elemental analysis, IR, 1H NMR, 31P NMR, and MS. Their antitumor activity against KB and CNE1 cells was examined. Some of the compounds showed potential antitumor activity, which provided some hints for further study of structure modification. In particular, the compounds 6i and 6j displayed more potent cytotoxic activities against KB in comparison with 5-FU. [Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Table S1] GRAPHICAL ABSTRACT
语种:
英文
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Efficient synthesis of fused pyrimidine derivatives with biological activity via Aza-Wittig reaction
作者:
Ren Qingyun;Tan Xiaosong;He Hongwu*
期刊:
Current Organic Synthesis ,2011年8(5):752-763 ISSN:1570-1794
通讯作者:
He Hongwu
作者机构:
[Ren Qingyun; He Hongwu; Tan Xiaosong] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[He Hongwu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
Fused pyrimidine derivatives;synthesis;aza-Wittig reaction;pharmaceutical activity;herbicidal activity;fungicidal activity;pyrido[4,3-d]pyrimidine-4(3H)-ones;3,4-dihydro-pyrido[4,3-d] pyrimidine-8-carbonitriles;pyrazolo[3,4-b]pyrido[4,3-d]-pyrimidine-4-ones;thieno[3',2'-5,6]pyrido [4,3-d]pyrimidin-4(3H)-ones;1,2,3-triazolo[4,5-d]pyrimidin-7-ones;1,2,4-triazolo[1,5-a]pyrimidin- 10(3H)-ones;thiazolo[4,5-d] pyrimidin-4(3H)-ones;pyrazolo[4',3':5,6] pyrano[2,3-d]pyrimidin-4 (3H)-ones
摘要:
Pyrimidine derivatives have played an important role in the chemistry of biological systems. This review focuses on recent work of our studies on the synthesis and biological activity of fused pyrimidine derivatives including pyrido[4,3-d]pyrimidine-4(3H)-ones; 3,4-dihydro-pyrido[4,3-d]pyrimidine-8-carbonitriles; pyrazolo[3,4-b]pyrido[4,3-d]-pyrimidine-4-ones; thieno[3',2'-5,6]pyrido [4,3- d]pyrimidin-4(3H)-ones; 1,2,3-triazolo[4,5-d]pyrimidin-7-ones; 1,2,4-triazolo[1,5-a]pyrimidin-10(3H)-ones; thiazolo[4,5-d]pyrimidin- 4(3H)-ones and pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidin-4(3H)-ones. The different approaches for the syntheses of these fused pyrimidine derivatives are described and reviewed. Parts of other researchers' most relevant work were also included in this review. © 2011 Bentham Science Publishers Ltd.
语种:
英文
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Synthesis, Characterization and X-ray Crystal Structure of N,N-Bis(4-nitrophenylcarba-mothioyl)-isophthalamide·DMF
作者:
Wang Hai-Qin;Chen Le;Peng Hao* ;He Hong-Wu
期刊:
Chinese Journal of Structural Chemistry ,2011年30(12):1765-1769 ISSN:0254-5861
通讯作者:
Peng Hao
作者机构:
[Peng Hao] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Peng Hao] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
关键词:
X-ray crystallography;acylthiourea;isophthaloyl
摘要:
A new crystal of N,N-bis(4-nitrophenylcarbamothioyl)isophthalamide DMF solva- te has been prepared at room temperature and characterized by elemental analysis and IR, MS, ~1H NMR spectra and X-ray single-crystal determination. The complex crystallizes in monoclinic, space group P2_1/c with a = 11.2093(12), b = 22.081(2), c = 13.9640(15) A,,,,= 112.128(2)°,1V = 3201.8(6) A~3, C_(28)H_(30)N_8O_8S_2, M_r = 670.72, Dc = 1.391 Mg/m~3, Z = 4,,,= 0.228 mm~(-1), F(000) = 1400, the final R = 0.0483 and wR = 0.1411 (I > 2>(I)). The molecular packing in the crystal is the result of N–H···O hydrogen bonding.
语种:
英文
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塑料磷系阻燃剂研究与应用
作者:
贺红武;张翔宇;黄琰;游歌云
作者机构:
华中师范大学化学学院有机合成研究所
会议名称:
2011国际精细磷化工技术交流大会
会议时间:
2011-05-01
会议地点:
成都
会议论文集名称:
2011国际精细磷化工技术交流大会论文集
关键词:
磷系阻燃剂;耐燃性能;塑料制品;使用安全性能
摘要:
阻燃剂的作用是阻止材料引燃或抑制火焰传播。橡胶和塑料等高分子材料的耐热和耐燃性能较差,阻燃剂可提高橡塑制品的使用安全性能,因此成为橡塑制品加工的重要添加剂之一。本文介绍了国内外阻燃剂的发展状况及趋势,着重讨论了应用于塑料的磷系阻燃剂的研究进展。
语种:
中文
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Synthesis and biological evaluation of novel (Thio)urea derivatives as potential antitumor agents
作者:
Jin, Chuanfei;Liang, Yong-Ju;He, Hongwu* ;Fu, Liwu
期刊:
Archiv der Pharmazie ,2011年344(11):741-744 ISSN:0365-6233
通讯作者:
He, Hongwu
作者机构:
[He, Hongwu; Jin, Chuanfei] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan, Peoples R China.;[Liang, Yong-Ju; Fu, Liwu] Sun Yat Sen Univ, Ctr Canc, State Key Lab Oncol S China, Guangzhou 510275, Guangdong, Peoples R China.;[He, Hongwu] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, 152 Luoyu Rd, Wuhan, Peoples R China.
通讯机构:
[He, Hongwu] C;Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, 152 Luoyu Rd, Wuhan, Peoples R China.
关键词:
Antitumor activity;Pyrimidinyl group;Thiourea;Urea
摘要:
A series of novel (thio)ureas containing the pyrimidinyl group was designed and synthesized. Their in-vitro antitumor activity against different human tumor cells was examined. Some of the compounds showed potential antitumor activity, which provided some hints for further studies on structure modification. A series of novel (thio)urea derivatives was designed and synthesized. The in-vitro preliminary bioassay data showed that compound 4k was found to have more potent cytotoxic activities against some human tumor cells than 5-FU. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
语种:
英文
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