共查询到19条相似文献,搜索用时 97 毫秒
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10-酯基高喜树碱的全合成及抗肿瘤活性研究 总被引:2,自引:0,他引:2
以2,8-二氧-3-乙基-6,6-亚乙二氧基-2,3,5,6,7,8-六氢-3-羟基吡喃(5,4-c)中氮茚为起始原料, 经五步反应得到高喜树碱, 羟甲基化后与一系列酸成酯合成了6个10-酯基高喜树碱, 并利用1H NMR, MS及元素分析对其结构进行了表征. 采用经典的噻唑兰(Thiazoly blue tetrazolium bromide, MTT)法测定了其体外抗肿瘤活性, 活性测试结果表明3个化合物具有比阳性对照药拓扑替康增强的活性. 相似文献
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The voltammetric behavior of camptothecin (CPT) in Britton-Robinson (B-R) buffer solutions (pH 2.09-9.07) was studied by the means of linear sweep voltammetry (LSV), cyclic voltarnmetry (CV) and normal pulse voltammetry (NPV) at a hanging mercury drop electrode. In different pH range of B-R buffer solutions, CPT could cause three reduction waves. In B-R buffer solutions (pH 2.09-5.46), wave P1 yielded by CPT was a two-electron wave. Between pH 6.01 and 9.07, CPT could yield two reduction waves P2 and P3. In addition, the pure CPT obtained from camptotheca acumina grown only in China was determined by NPV, and a linear response was observed in the range of 2.0 × 10^-3-4.0 × 10^-2 mmol·L^-1 with a 0.9991 correlation coefficient and a 8.0 × 1^-4 mmol·L^-1 detection limit for CPT. 相似文献
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To improve the biological anticancer activity of 20(S)-camptothecin, a novel class of 20(S)-20-O-camptothecin β-aminopropionates were designed and synthesized with camptothecins as the starting materials, through acylation with acryloyl chloride followed by Michael′s addition. Twelve esters, 1a-1d, 4a-4d and 5a-5d, were synthesized and evaluated by using MTT assay method. The results demonstrate that all these compounds show a potential cytotoxicity on KB, HT-29, HCT-8, and Bel7402 tumor cell lines. Some compounds, 1d, 4c, 5b, 5c and 5d, show a higher cytoto-xicity on KB and HCT-8 compared with camptothecin. 相似文献
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A novel synthesis to camptothecin is described. A Friedlander condensation of o-aminobenzaldehye 2 with tricylclic ketone 3 affords camptothecin after further elaboration. Tricyclic ketone 3 is prepared via a route employing a [3+2] nitrone cycloaddition and an intramolecular Knoevenagel condensation. 相似文献
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To characterize the pharmacokinetics of protein-free camptothecin in blood and brain we implanted microdialysis probes into the jugular vein and striatum of rats for unbound drug sampling and determination. Camptothecin (2 or 5 mg/kg, i.v., n=6) was then administered from the femoral vein, and microdialysates were collected from blood and brain of both sites and assayed by a validated microbore scale high-performance liquid chromatographic method. The mobile phase consisted of methanol–100 mM monosodium phosphoric acid (35:65, v/v, pH 2.5) with a flow-rate 0.05 ml/min. The fluorescence response for camptothecin was observed at excitation and emission wavelengths of 360 and 440 nm, respectively. Pharmacokinetic parameters were calculated from the corrected data for dialysate concentrations of camptothecin versus time. The results suggest that the pharmacokinetics of unbound camptothecin in blood and brain can be fitted best to a two- and one-compartment model, respectively. Camptothecin rapidly entered the extracellular fluid of brain striatum at 10 min following camptothecin administration. 相似文献
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Di Zao Li Xian Dao Pan Hong Yan Liu Song Wu 《中国化学快报》2008,19(10):1202-1205
A series of 5-C-alkylating camptothecins have been synthesized by one-step method, and their in vitro antitumor activity was evaluated against six human cancer cell lines. The results showed that all 5-C-alkylates of camptothecins possessed poor cytotoxicity on six human cancer cell lines. 相似文献
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Emilia Cupioli Frédéric J. M. Gaigne Anna Sachse Philipp Buday Prof. Dr. Wolfgang Weigand Dr. Phil Liebing Prof. Dr. Hans-Dieter Arndt 《Angewandte Chemie (International ed. in English)》2023,62(42):e202304901
Methanobactin OB3b (Mbn-OB3b) is a unique natural product with stunning affinity for copper ions (Ka≈Cu(I) 1034). Here, we report the first total synthesis of Cu(I)-bound methanobactin OB3b featuring as key transformations a cyclodehydration-thioacylation sequence, to generate the conjugated heterocyclic systems, and a copper-templated cyclization, to complete the caged structure of the very sensitive target compound. 相似文献
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Marie Devert 《Tetrahedron》2010,66(35):7227-2584
The first total synthesis of (±)-17-norcamptothecin, a novel camptothecin analog possessing an α-hydroxy-γ-lactone E-ring, has been accomplished by using a short and flexible route. The stability of this new compound in aqueous medium has been evaluated through fluorescence spectroscopy. 相似文献
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Bo Li Chuanzhen Tan Tianhao Ma Prof. Yanxing Jia 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2024,136(10):e202319306
We have achieved the first total synthesis of bipolarolides A and B, which possess an intriguing and complex 5/6/6/6/5 caged pentacyclic skeleton with seven contiguous stereocenters. The synthesis features a lithium-halogen exchange/intermolecular nucleophilic addition to link two enantioenriched fragments, two ring-closing metathesis reactions to assemble the five- and eight-membered rings, and a bioinspired Prins reaction/ether formation cascade cyclization to construct the 5/6/6/6/5 caged skeleton. 相似文献
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Steven H. Bennett Graeme Coulthard Varinder K. Aggarwal 《Chemical record (New York, N.Y.)》2020,20(9):936-947
Prostaglandins have been attractive targets in total synthesis for over 50 years, resulting in the development of new synthetic strategies and methodologies that have served the broader chemical community. However, these molecules are not just of academic interest, a number of prostaglandin analogues are used in the clinic, and some are even on the WHO list of essential medicines. In this personal account, we describe our own approach to the family of prostaglandins, which centers around the synthesis of a key enal intermediate, formed from the l ‐proline catalysed dimerization of succinaldehyde. We highlight the discovery and further optimization of this key reaction, its scale up, and subsequent application to a range of prostaglandins. 相似文献