共查询到20条相似文献,搜索用时 15 毫秒
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Tatsuro Ouchi Hirotoshi Fujie Satoshi Jokei Yoshiomi Sakamoto Hidenori Chikashita Takeshi Inoi Otto Vogl 《Journal of polymer science. Part A, Polymer chemistry》1986,24(9):2059-2074
Acryloyl-type polymer fixing 1-β-carbonylethyl-5-fluorouracil residues through D -glucofuranoses via ester bonds was synthesized by means of polymerization of the corresponding monomer and polymer reaction. In order to provide the water-soluble objective polymer, the copolymerization of the acryloyl-type monomer with acrylamide was carried out. The extent of release of 5-FU residues from the copolymer was investigated in the enzyme or nonenzyme system in vitro. Furthermore, the antitumor activities of the water-insoluble homopolymer and water-soluble copolymer obtained were tested in vivo. 相似文献
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Ozaki Shoichiro Kong Xiang-Zheng Watanabe Yutaka Hoshiko Tomonori Ogasawara Tomio Ueno Takao Furukawa Uiroyuki Iigo Masaaki Hoshi Akio 《中国化学》1998,16(2):171-177
In order to get good antitumor agents especially better than 5-fluorouracil, tegafur and l-hexylcarbamoyl-5-fluorouracil (HCFU), fourty nine 1-carbamoyl-5-fluorouracil having aromatic ring were synthesized from 5-fluorouracil and isocyanates or mines. Antitumor activity was tested in the L1210 tumor system, and 5 compounds gave better value of therapeutic ratio than 5-fluorouracil, tegafur, HCFU. 1-(4-Methoxybenzylcarbamoyl)-5-fluorouracil gave the best result. 相似文献
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N Amishiro S Nagamura E Kobayashi A Okamoto K Gomi H Saito 《Chemical & pharmaceutical bulletin》1999,47(10):1393-1403
A series of A-ring pyrrole compounds of duocarmycin bearing 5-membered heteroarylacryloyl groups (thienylacryloyl and pyrrolylacryloyl) and heteroarylcarbonyl groups were synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. Most of the thienylacrylates displayed in vitro anticellular activity equivalent to 4'-methoxycinnamates. Among the 8-O-[(N-methylpiperazinyl)carbonyl] derivatives of methoxy-thienylacrylates, compound 11b, having 4'-methoxy-2'-thienylacryloyl as segment-B (Seg-B), showed remarkably potent antitumor activity and low peripheral blood toxicity in vivo, which were equal to those of 8-O-[(N-methylpiperazinyl)carbonyl] derivatives of 4'-methoxycinnamates, compared with the A-ring pyrrole derivatives having the trimethoxyindole skeleton in Seg-B. On the other hand, the 2'-pyrrolylacrylates having a double bond as spacer showed 10(2)- to 10(3)-fold stronger anticellular activity than 2'-pyrrolecarboxylates (IC50 < 0.3 nM, 72 h-exposure). The 8-O-acetate and 8-O-[(N-methylpiperazinyl)carbonyl] derivatives of 2'-pyrrolylacrylates exhibited an antitumor effect at a lower dose compared with the 8-O-[(N-methylpiperazinyl] derivatives of 4'-methoxycinnamate (1j). Moreover, it was expected that the antitumor activity would be increased by the strength of the extra hydrogen bond formed between the nitrogen of the pyrrole amido group and DNA, owing to the increase of the number of N-methyl-2'-pyrrolecarboxamide units. However, 2'-pyrrolylacrylates having three N-methyl-2'-pyrrolecarboxamide units showed nearly equal antitumor activity to 2'-pyrrolylacrylates having only one N-methyl-2'-pyrrolecarboxamide unit. 相似文献
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This paper describes the synthesis of two series of rigid macrocycles from hydrogen bonding-induced folded aryl amide and hydrazone oligomers that bear two amines or one amine and one aldehyde. The diamines reacted with diacyl chloride to produce amide macrocycles, whereas the latter underwent self-coupling reactions to afford imine macrocycles. DFT calculations revealed that the new macrocycles possess rigid planar conformations and their cavity diameters were estimated to be 1.86 nm–2.75 nm. 相似文献
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With the aim of diminishing the toxicity of 5-fluorouridine (1) and obtaining biologically active derivatives of 1, various kinds of 5'-O-acyl-5-fluorouridines 2 were synthesized. The antitumor activity of the compounds against L-1210 leukemia in mice was examined. The 5'-O-heptanoyl derivative 2h showed the highest antitumor activity. 相似文献
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S Ozaki T Akiyama T Morita M Kumegawa T Nagase N Uehara A Hoshi 《Chemical & pharmaceutical bulletin》1990,38(11):3164-3166
Various kinds of 5'-O-unsaturated acyl 5-fluorouridines were synthesized to obtain 5-fluorouridine derivatives with low toxicity and high antitumor activity. Antitumor activity of the compounds against L-1210 leukemia in mice was examined, and the 5'-O-4-pentenoyl derivative showed the highest antitumor activity. 相似文献
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Guey‐Sheng Liou Sheng‐Huei Hsiao 《Journal of polymer science. Part A, Polymer chemistry》2002,40(4):459-470
Two series of phosphorus‐containing aromatic poly(ester amide)s with inherent viscosities of 0.46–3.20 dL/g were prepared by low‐temperature solution polycondensation from 1,4‐bis(3‐aminobenzoyloxy)‐2‐(6‐oxido‐6H‐dibenz〈c,e〉〈1,2〉oxaphosphorin‐6‐yl)naphthalene and 1,4‐bis(4‐aminobenzoyloxy)‐2‐(6‐oxido‐6H‐dibenz〈c,e〉〈1,2〉oxaphosphorin‐6‐yl)naphthalene with various aromatic diacid chlorides. All the poly(ester amide)s were amorphous and readily soluble in many organic solvents, such as N,N‐dimethylformamide, N,N‐dimethylacetamide (DMAc), and N‐methyl‐2‐pyrrolidone (NMP). Transparent, tough, and flexible films of these polymers were cast from DMAc and NMP solutions. Their casting films had tensile strengths of 71–214 MPa, elongations to break of 5–10%, and initial moduli of 2.3–6.0 GPa. These poly(ester amide)s had glass‐transition temperatures of 209–239 °C (m‐series) and 222–267 °C (p‐series). The degradation temperatures at 10% weight loss in nitrogen for these polymers ranged from 462 to 489 °C, and the char yields at 800 °C were 55–63%. Most of the poly(ester amide)s also showed a high char yield of 35–45%, even at 800 °C under a flow of air. The limited oxygen indices of these poly(ester amide)s were 35–46. © 2002 John Wiley & Sons, Inc. J Polym Sci Part A: Polym Chem 40: 459–470, 2002; DOI 10.1002/pola.10129 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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Synthesis and antitumor activity of novel 10-amino acids ester homocamptothecin analogues 总被引:2,自引:0,他引:2
Liang You Wan Nian Zhang Zhen Yuan Miao Wei Guo Xiao Ying Che Wen Ya Wang Chun Quan Sheng Jiang Zhong Yao Ting Zhou 《中国化学快报》2008,19(7):811-813
Nine racemic homocamptothecin derivatives were synthesized and in vitro antitumor activities were evaluated by standard MTT method. The results showed that some of the compound had higher antitumor activity than iritecan. 相似文献
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Shehadeh Mizyed Muhammad Ashram 《Journal of inclusion phenomena and macrocyclic chemistry》2011,70(1-2):135-142
A series of acyclic Schiff base podands 14?C19 with lipophilic amide and ester end groups were synthesized in good yield and in a simple way. Their transition metal ions complexation was studied using conductometric method in acetonitrile (AN) at 25 °C. Schiff base podands 14?C16 showed a continuous decrease in the molar conductances in their complexation with Hg2+, Pb2+, Cu2+, Zn2+ and Cd2+ which begins to level off at a mole ratio of 1:1 crown-to-metal indicating the formation of a stable 1:1 complexes. The order of the stability constants of the metal ions studied with the Schiff base podands 14, 15 and 16 is: Hg2+ > Pb2+ > Cu2+ > Zn2+ > Cd2+ > Ag+. Metal ion complexation by acyclic diamide or diester podands involves presumably the oxygen atoms of the carbonyl groups in addition to the nitrogen atoms of the imino groups. 相似文献
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A linear and a branched nonionic cleavable surfactants containing a carbonate bond have been prepared from tetra(ethylene glycol) and an alkylchloroformate. The stability of these carbonate surfactants was determined by investigating their hydrolysis and biodegradability characteristics. The hydrolysis was catalyzed by alkali or enzymes (esterase from porcine liver and lipases from Mucor miehei and Candida antarctica B) and was monitored using 1H NMR. It was found that the stability toward alkali was higher for a carbonate surfactant than for a corresponding surfactant with an ester as weak bond. Biodegradation tests resulted in more than 60% degradation after 28 days for both carbonate surfactants. Physicochemical properties, such as critical micelle concentration (CMC), cloud point, area per molecule, and surface tension at the CMC, were determined and compared to those obtained from similar surfactants containing ester, amide, or ether bonds. It was found that the carbonate linkage is hydrophobic and that the oxycarbonyl part of the carbonate group is equivalent, in a formal sense, to an extra methylene group in the alkyl chain of the surfactant. 相似文献
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R. A. Zhuk A. S. Ludzisha E. G. Shpaer M. Yu. Lidak A. A. Zidermane D. V. Meirena 《Chemistry of Heterocyclic Compounds》1985,21(10):1159-1163
1-(3-Phthalidyl)-5-fluorouracils were synthesized by alkylation of 2,4-bis(trimethylsilyl)-5-fluorouracil with substituted 3-bromophthalides, and the rate constants for hydrolysis at pH 8.0–11.5 were determined. The antineoplastic activity of a number of the compounds was established, and it was assumed that there is a relationship between the biological activity and the rate of hydrolysis.See [1] for communication 18.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1406–1411, October, 1985. 相似文献
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Mael Nicolas Frédéric Guittard Serge Géribaldi 《Journal of polymer science. Part A, Polymer chemistry》2007,45(20):4707-4719
A series of new fluorinated polythiophenes has been synthesized by oxidative chemical and electrochemical polymerization and by Ullmann coupling. The substitution with the perfluoroalkyl alkyl chain CH2CH2C6F13 on the 3 position of the thiophene ring is performed via an ester, thioester, or amide connector, (CH2)m‐C(O)X, m = 0–2, with a view to investigating the role of the linker on the polymerization and on the properties of the corresponding polymers. The bromination of the monomers at the 2 and 5 positions allows the use of Ullmann coupling to form soluble fluorinated oligomers. The electron affinity was determined from cyclic voltammetry and a value of 3.1 eV was found for the ester derivative; such materials represent interesting candidates for use in light‐emitting devices or as an electron accepting material in photodiodes/solar cells. The oxidative polymerizations need the connector to be spaced out from the heterocycle to reduce its withdrawal effect. The ester, thioester, and amide spacer determined to a large extent the efficiency of the oxidative polymerization, and particularly the electropolymerization, as well as the solubility of the polymers formed. All the polymers were analyzed by GPC and by UV–visible and fluorescence spectroscopies. The electrochemical oxidation of the thioester and amide group prevents the formation of electroactive films by electropolymerization. But in the case of the ester group, the electroformed polymer exhibits exceptional stable superhydrophobic and lipophobic properties because of a porous surface and the presence of a fluorinated chain that confers low surface energy. © 2007 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 45: 4707–4719, 2007 相似文献
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