共查询到20条相似文献,搜索用时 140 毫秒
1.
5-氟尿嘧啶N1-甲酰基氨基酸、短肽的合成及抗肿瘤活性 总被引:4,自引:0,他引:4
5-氟尿嘧啶N1-甲酰氯分别与Gly、Val、Leu、Ile、Phe、Asp和Glu的苄酯反应,制备了7种5-氟尿嘧啶-N1-甲酰基氨基酸苄酯。氢解后得到了相应的5-氟尿嘧啶N1-甲酰氨基酸。将其进一步与氨基酸甲酯或二肽甲酯缩合,制备了5-氟尿嘧啶N1-甲酰基二肽甲酯和三肽甲酯。5-氟尿嘧啶-N1-甲酰基二肽甲酯也可采用5-氟尿嘧啶-N1-甲酰氯与二肽甲酯直接反应制备。 相似文献
2.
氨基酸5—氟尿嘧啶酯类衍生物的合成及其抗肿瘤活性研究 总被引:1,自引:0,他引:1
用氨基酸作抗癌药物载体以提高对癌细胞选择性的研究引起了人们的浓厚兴趣。在前文中,我们报道了5-氟尿嘧啶乙酰和丙酰氨基酸及其氨基酸的3-(N′-5-氟尿嘧啶基)-丙醇酯的合成及其抗肿瘤试验研究。本文将报道一系列氨基酸(5-氟尿嘧啶-1,3-双丙基)酯盐酸盐的合成及其体外抗肿瘤活性的研究。 合成路线如下: 相似文献
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含5-氟尿嘧啶生物可降解聚磷酰胺的合成及其抗肿瘤活性研究 总被引:2,自引:0,他引:2
通过L-赖氨酸(N1-5-氟尿嘧啶)烷基酯双盐酸盐与二氯磷酸乙酯、二氯膦甲酸乙酯、二氯膦乙酸乙酯共聚,合成了三类12种侧链含5-氟尿嘧啶的聚磷酰胺。聚合物的结构经UV、IR、1H NMR及元素分析鉴定。聚合物用微量细胞培养四氮唑实验方法(MTT法)进行了对人肝癌细胞系Bel-7402细胞的微量培养实验。 相似文献
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以2-乙氧基乙胺和3-氯-1-丙醇等为起始原料, 经7步反应, 制备了N,N-二[二(3-甲氧基丙基)膦基乙基]-2-乙氧基乙胺(PNP5)盐酸盐, 其中关键步骤是后两步. PNP5盐酸盐的结构和组成通过IR, 1H NMR, 13C NMR, 31P NMR, MS和元素分析等方法确认. 相似文献
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5-氟尿嘧啶是一种广谱性的抗肿瘤药物, 其缺点是脂溶性小, 毒副作用较大, 为此, 对该化合物进行了大量的化学修饰工作, 本文通过2,4,-双三甲硅基-5-氟尿嘧啶分别与乙酸-W-溴代烷基酯和α-溴代丙二酸二乙酯的反应, 然后醇解, 制备了五种N'羟烷基-5-氟尿嘧啶-(2a-e)和α-5-氟尿嘧啶-N'-丙二酸二乙酯(3), 通过5-氟尿嘧啶与衣康酸二甲酯反应, 制备了α-5-氟脲嘧啶-N'-甲基丁二酸二甲酯(4)。将以上所得到的两种α-5-氟尿嘧啶-N'-二羧酸酯水解, 制得α-5-氟尿嘧啶-N'-丙二酸(5)和α-5-氟尿嘧啶-N'-甲基丁二酸(6)。 相似文献
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信使RNA(Messenger RNA, mRNA)上存在众多修饰,包括N6-甲基腺嘌呤修饰(N6-methyladenosine, m6A)、N1-甲基腺嘌呤修饰(N1-methyladenosine, m1A)及胞嘧啶甲基化(5-methylcytosine, m5C)等.其中, m6A是mRNA内部修饰碱基中占比最高的一种,影响着mRNA的5′和3′端加工、在细胞中的定位、降解和翻译等过程,并在转录后调控基因表达水平,以此参与胞内的多种生理活动.本文综合评述了m6A修饰的分子机制及其与多种疾病的关系,概述了m6A鉴定技术的发展历程,重点讨论了m6A化学干预的最新研究进展,以期让读者全面了解m6A修饰,并为后续开发针对m6A修饰的小分子药物提供参考. 相似文献
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?rt Malavaši?Uroš Grošelj Amalija Golobi?Jure Bezenšek Branko Stanovnik Katarina Stare Jernej WaggerJurij Svete 《Tetrahedron: Asymmetry》2011,22(6):629-640
Eleven (S)-1,6-dialkylpiperazine-2,5-diones and five (3S,6S)-1,3,6-trialkylpiperazine-2,5-diones were prepared in three steps from the corresponding (S)-α-amino acid esters comprising of reductive N-alkylation, N-acylation and cyclisation. The synthesis of (S)-1,6-dialkylpiperazine-2,5-diones has a broad scope allowing preparation of diketopiperazines with primary and secondary alkyl groups at N(1), while the synthesis of (3S,6S)-1,3,6-trialkylpiperazine-2,5-diones is limited to compounds with primary alkyl groups at N(1). Reductive alkylation of amino acid ester hydrochlorides by catalytic hydrogenation in the presence of a carbonyl compound proved to be a simple, efficient and general method for the preparation of stable (storable) α-alkylamino acid ester hydrochlorides. The structures of the novel compounds were determined by NMR and X-ray diffraction. 相似文献
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Kireeva D. R. Zileeva Z. R. Ishmetova D. V. Dokichev V. A. 《Russian Journal of Organic Chemistry》2021,57(7):1180-1183
Russian Journal of Organic Chemistry - The reaction of ethyl benzoylacetate with formaldehyde and natural amino acid ester hydrochlorides in acetate buffer (AcONa/AcOH, pH 4.0) at room temperature... 相似文献
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Yasumasa Hamada 《Chemical record (New York, N.Y.)》2014,14(2):235-250
This review describes our recent works on the diastereo‐ and enantioselective synthesis of anti‐β‐hydroxy‐α‐amino acid esters using transition‐metal–chiral‐bisphosphine catalysts. A variety of transition metals, namely ruthenium (Ru), rhodium (Rh),iridium (Ir), and nickel (Ni), in combination with chiral bisphosphines, worked well as catalysts for the direct anti‐selective asymmetric hydrogenation of α‐amino‐β‐keto ester hydrochlorides, yielding anti‐β‐hydroxy‐α‐amino acid esters via dynamic kinetic resolution (DKR) in excellent yields and diastereo‐ and enantioselectivities. The Ru‐catalyzed asymmetric hydrogenation of α‐amino‐β‐ketoesters via DKR is the first example of generating anti‐β‐hydroxy‐α‐amino acids. Complexes of iridium and axially chiral bisphosphines catalyze an efficient asymmetric hydrogenation of α‐amino‐β‐keto ester hydrochlorides via dynamic kinetic resolution. A homogeneous Ni–chiral‐bisphosphine complex also catalyzes an efficient asymmetric hydrogenation of α‐amino‐β‐keto ester hydrochlorides in an anti‐selective manner. As a related process, the asymmetric hydrogenation of the configurationally stable substituted α‐aminoketones using a Ni catalyst via DKR is also described. 相似文献
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A. A. F. Wasfy 《Phosphorus, sulfur, and silicon and the related elements》2013,188(5):1349-1358
The reaction of quinazoline-4(3H)-thiones 2a-d with amino acid ester hydrochlorides in boiling solvents, under the basic catalysis, afforded the corresponding substitution products (3-6)a-e in low yield. The reaction could be improved by carrying it without a solvent yielding imidazo[1,2-c]- and pyrimido[1,2-c]quinazolines (7-10)a-e . The antibacterial and antifungal activities of the prepared compounds were tested. 相似文献
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A. V. Lebedev A. B. Lebedeva V. D. Sheludyakov V. V. Shatunov S. N. Ovcharuk 《Russian Journal of General Chemistry》2007,77(4):581-585
Treatment of an alcoholic suspension of amino acids with trimethylchlorosilane yielded phenylglycine, valine, β-phenylalanine, and homovaline ester hydrochlorides. Their saccharin-catalyzed silylation with hexamethyldisilazane proceeds quantitatively and involves only one proton of the amino group. The best conversion of the amino acid esters to the corresponding isocyanates was achieved by phosgene treatment of their monosilyl urethanes, rather than of the silylated amino esters. Monosilyl urethanes are formed quantitatively by treatment of the amino acid ester hydrochlorides with the hexamethyldisilazane-CO2 system. The 1H NMR spectra show that monosilyl urethanes derived from α-and β-amino acid esters are characterized by intramolecular interaction of the silicon atom and the oxygen atom of the carboxy group. 相似文献
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含5-氟尿嘧啶的氨基酸衍生物的合成及其抗肿瘤活性研究 总被引:2,自引:0,他引:2
5-氟尿嘧啶乙酸对硝基苯酯和5-氟尿嘧啶丙酸对硝基苯酯与一系列氨基酸反应,制备了12个新的含5-氟尿嘧啶的氨基酸衍生物,并确定了化合物的结构。初步动物试验表明某些化合物有一定的抗肿瘤活性。 相似文献
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Yuan Chen Lulu Fu Baobao Sun Cheng Qian Dr. Srikala Pangannaya Hong Zhu Prof. Jing Ma Prof. Juli Jiang Dr. Zhigang Ni Prof. Ruibing Wang Prof. Xiancai Lu Prof. Leyong Wang 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(19):5890-5896
Chiral α-amino acids play critical roles in the metabolic process in nearly all life forms. So far, chiral recognition of α-amino acids has mainly focused on the determination of l /d enantiomers. Herein, selection of planar chiral conformations between water-soluble pillar[5]arene WP5 and pillar[6]arene WP6 was observed due to α-side chain or ethyl ester moieties of l -α-amino acid ethyl ester hydrochlorides binding with WP5 and WP6 , respectively. Therefore, α-side chain and ethyl ester moieties of l -α-amino acid ethyl ester hydrochlorides were recognized by observing the induced CD signal and its inversion. This is a rare example of being able to detect the chiral region around α-carbon of a chiral α-amino acid molecule. 相似文献
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Two substituted quinazolinyl/imidazolyl-salicylic acids 5, 6 were synthesized by the reaction of 6-iodo-2-methylbenzoxazin-4-one/5-nitroimidazole with 5-aminosalicylic acid (5-ASA). Coupling of compounds 5 and 6 with different amino acid ester hydrochlorides, dipeptide and tripeptide methyl esters yielded novel quinazolino/imidazolopeptide derivatives 5a-f and 6a-g. The chemical structures of all newly synthesized compounds were confirmed by means of FT-IR, (1)H- and (13)C-NMR, MSand elemental analysis. Selected peptide ester derivatives were further hydrolyzed by using lithium hydroxide (LiOH) to afford the corresponding acid derivatives 5ba-da and 6e(a)-g(a). All peptide derivatives were assayed for antimicrobial and anthelmintic activities against eight pathogenic microbes and three earthworm species. Among the tested compounds, 5e,5d, 6e and their hydrolyzed analogs 5d(a) and 6e(a) exhibited higher antimicrobial activity against Pseudomonas aeruginosa, Klebsiella pneumoniae and Candida albicans, and 5(a),6g and 6g(a) displayed better antifungal activity against the dermatophytes Trichophyton mentagrophytes and Microsporum audouinii. Moreover, 6f and its hydrolyzed derivative6f(a) showed good anthelmintic activity against Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugeniea at dose of 2 mg mL(-1). 相似文献
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Several amino acid ester hydrochlorides were reacted with ammonium formate to give N-formyl amino acid esters in good yields. 相似文献
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《Journal of heterocyclic chemistry》2017,54(6):3481-3489
A series of 1‐[(4‐hydroxy‐2‐oxo‐1‐phenyl‐1,2‐dihydroquinolin‐3‐yl)carbonyl]‐4‐(substituted) piperazines 3a–c and methyl 2‐[(4‐hydroxy‐2‐oxo‐1‐phenyl‐1,2‐dihydroquinolin‐3‐yl)carbonylamino] alkanoates 5a–d has been developed by the direct condensation of ethyl [4‐hydroxy‐2‐oxo‐1‐phenyl‐1,2‐dihydro‐3‐quinoline] carboxylate 2 with N 1‐monosubstituted piperazine hydrochlorides or amino acid ester hydrochloride in the presence of triethyl amine. The quinolone amino acid esters 5a–d were the key intermediate for the preparation of a series of 1‐[2‐((4‐hydroxy‐2‐oxo‐1‐phenyl‐1,2‐dihydroquinolin‐3‐yl)carbonylamino)alkylcarbony]‐4‐substituted piperazine derivatives 8–11 (a‐d) via azide coupling method with amino acid ester hydrochloride. 相似文献