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1.
The synthesis of neopeltolide analogues that contain variations in the oxazole-containing side chain and in the macrolide core are reported along with the GI(50) values for these compounds against MCF-7, HCT-116, and p53 knockout HCT-116 cell lines. Although biological activity is sensitive to changes in the macrocycle and the side chain, several analogues displayed GI(50) values of <25 nM. Neopeltolide and several of the more potent analogues were significantly less potent against p53 knockout cells, suggesting that p53 plays an auxiliary role in the activity of these compounds. 相似文献
2.
Stéphanie Ballereau Nathalie Andrieu-AbadieNathalie Saffon Yves Génisson 《Tetrahedron》2011,67(14):2570-2578
Six new aziridine-containing analogs of phytosphingosine designed as constrained anhydrophytosphingosine were synthesized. The synthetic route developed also afforded an access to an original bicyclic analog of the natural anhydrophytosphingosine jaspine B. All these new compounds were evaluated for their capacities to affect melanoma cell viability. 相似文献
3.
A. E. Shipov O. I. Artyushin G. K. Genkina A. V. Khrunin O. Yu. Eremina E. I. Bakanova S. A. Roslavtseva T. A. Mastryukova 《Russian Chemical Bulletin》2000,49(9):1593-1597
Methods were developed for the synthesis of 2-butylthio-2-oxo-1,3,2-oxazaphosphorinane, 2-butylthio-2-thioxo-1,3,2-dioxaphosphorinane, and 2-butylthio-2-thioxo-1,3,2-diazaphosphorinane, as well as of acyclicS-butylO-ethyl (diethylamido)phosphorothioates and-dithioates andS-butyl bis(diethylamido)phosphorodithioate. These compounds can serve as models of possible metabolites of cyclic compounds. Based on the data obtained in studies of the antiesterase activity of the resulting compounds and their synergistic activity in mixtures with permethrine, a possible mechanism ofin vitro andin vivo biological action of diheteraphosphorinanes was proposed. 相似文献
4.
Kim HO Baek HW Moon HR Kim DK Chun MW Jeong LS 《Organic & biomolecular chemistry》2004,2(8):1164-1168
tert-Azido or amino substituted penciclovir analogs, 1-3 were synthesized for the purpose of improving the efficacy and bioavailability of penciclovir and searching for novel antiviral agents. Among several methods attempted to insert an azido group into the alpha,beta-unsaturated ester 6, only Bronsted acid-catalysed 1,4-conjugate addition conditions (NaN3, 75% acetic acid, 80 degrees C) gave the desired tert-azido product 7. The synthesized final penciclovir analogs 1-3 were evaluated in vitro against several viruses such as HIV-1, HSV-1 and 2, poliovirus, VZV, and VSV. Compound 2 only showed weak antiviral activity against HSV-1 without cytotoxicity. Although the synthesized compounds did not exhibit an excellent antiviral activity, the successful method used in introducing the tert-azido group is expected to be generally utilized for the synthesis of nucleoside analogs with a tert-azido substituent. 相似文献
5.
Dapagliflozin is currently the most advanced SGLT2 inhibitor, which has been used in Phase III clinical trials for treatment of diabetes. Here we describe the design and synthesis of Dapagliflozin analogs modified with gem-difluoromethylene group. Their biological evaluation of in vitro inhibitory activity against human SGLT2 showed that some of the analogs with CF2 at C-4 are better SGLT2 inhibitors compared with Dapagliflozin. 相似文献
6.
Eguchi T Kanai S Kakinuma K Okazaki T Mizoue K 《Chemical & pharmaceutical bulletin》2000,48(10):1470-1473
A novel potentiator of nerve growth factor (NGF), NG-061, which had been isolated from the fermentation broth of Penicillium minioluteum F-4627, was synthesized from methoxybenzoquinone and phenylacetylhydrazine in a single step. A series of acyl hydrazone derivatives were also synthesized and their potentiator activity of neurotrophic effect of NGF on neurite outgrowth was evaluated by assay with a rat pheochromocytoma cell line PC12. 相似文献
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Several structural analogs that contain only part of the altohyrtin structure have been prepared and compared with synthetic altohyrtin C (2) for in vitro cytotoxicity against human colon (HCT116) and ovarian (A2780) cell lines. Whereas altohyrtin C was found to be exceedingly potent against these lines (IC50=0.0003 μM), analogs 3-5 were >27,000-fold less potent (IC50>8 μM). Analogs 6 and 7 also demonstrated weak cytotoxicity with IC50 values for the HCT116 and A2780 cells of 4.8 μM and 2.4 μM, respectively, for 6. 相似文献
9.
Thota GaneshJennifer K Schilling Radha K PalakodetyRudravajhala Ravindra Natasha ShankerSusan Bane David G.I Kingston 《Tetrahedron》2003,59(50):9979-9984
The two fluorescently labeled epothilones 14 and 15 have been synthesized using a modification of Nicolaou's macrolactonization and Stille coupling strategy. The cytotoxicities of the compounds were 6.1 and 2.7 μg/mL, respectively, against the A2870 ovarian cancer cell line, and 0.5 and 1.0 μg/mL, respectively, against the PC-3 prostate cancer cell line. The critical concentration of tubulin was 0.5 and 1.0 μM in the presence of 14 and 15, respectively, compared with 0.3 μM for paclitaxel. The fluorescent properties of the two molecules in solution and bound to microtubules are described. 相似文献
10.
Mycalolide analog 4, consisting only of the side chain of mycalolide B (2), a trisoxazole macrolide of marine origin, was stereoselectively synthesized using Roush crotylboration, an Evans aldol reaction, and a Paterson aldol reaction as key steps. The analog 4 was found to have strong actin-depolymerizing activity. 相似文献
11.
Inamura S Fujimoto Y Kawasaki A Shiokawa Z Woelk E Heine H Lindner B Inohara N Kusumoto S Fukase K 《Organic & biomolecular chemistry》2006,4(2):232-242
The peptidoglycan (PG) bacterial cell wall glycoconjugate has been well known as a strong immunopotentiator. Partial structures of PG were chemically synthesized for elucidation of precise biological activities. Effective construction of distinct repeating glycans of PG was accomplished by the coupling of a key disaccharide glucosaminyl-beta(1-4)-muramic acid unit. Stereoselective glycosylation of disaccharide units was achieved by neighboring group participation of the N-Troc (Troc = 2,2,2-trichloroethoxycarbonyl) group and appropriate reactivity of N-Troc-glucosaminyl trichloroacetimidate. By using an efficient synthetic strategy, mono-, di-, tetra- and octasaccharide fragments of PG were synthesized in high yields. The biological activity of synthetic fragments of PG was evaluated by induction of tumor necrosis factor-alpha (TNF-alpha) from human monocytes, and toll-like receptor 2 (TLR2) and Nod2 dependencies by using transfected HEK293 cells, respectively. Here we reveal that TLR2 was not stimulated by the series of synthetic PG partial structures, whereas Nod2 recognizes the partial structures containing the MDP moiety. 相似文献
12.
《Tetrahedron letters》2014,55(52):7226-7228
A new series of febrifuginol analogues was prepared from l-glutamic acid. An antimalarial activity evaluation against chloroquine-sensitive (T96) and chloroquine-resistant (K1) Plasmodium falciparum indicated that all the tested compounds had very strong inhibitory activity. Compounds 4 and 17b′ were inactive against KB, MCF7, HepG2 and LU1 cell lines even at a concentration of 100 μM, while they exhibited significant inhibition towards P. falciparum. Comparison of the antimalarial activity and the cytotoxic properties revealed that the 2′S isomers were more active than the corresponding 2′R isomers for this series of febrifuginol analogues, indicating that the C-2′ position is critical for the biological activity of this class of compounds. 相似文献
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14.
[reaction: see text] Potassium bromo- and iodomethyltrifluoroborates have been prepared via in situ reaction of n-BuLi with dibromo- and diiodomethane, respectively, in the presence of trialkyl borates, followed by treatment with KHF(2). Moreover, a new synthetic method for the preparation of potassium organotrifluoroborates through nucleophilic substitution of the halide in these potassium halomethyltrifluoroborates is described. 相似文献
15.
The review summarizes data on the synthesis and properties of analogs of ABBB-and ABAB-type tetrapyrrole macrocycles and their
metal complexes. The structural features of these compounds are discussed. Data on aromaticity and biological properties are
considered.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 4, pp. 663–679, April, 2007. 相似文献
16.
T. N. Gribanova R. M. Minyaev A. G. Starikov V. I. Minkin 《Russian Chemical Bulletin》2009,58(4):691-705
The structures and stability of complexes of transition metal tricarbonyls (M = Co, Fe, Mn, Cr) with hydrocarbon and borane
basal rings, (C
n
H
n
)M(CO)3 and (B
n
H
2n
)M(CO)
n
, respectively, as well as internal rotation of the metal tricarbonyl fragments in these systems were studied by the DFT B3LYP/6-311+G(df,p)
method. Replacement of hydrocarbon basal fragments by isoelectronic borane rings leads to strengthening of the interaction
between the apical and basal fragments, but does not change the trend in the heights of barriers to internal rotation. In
all cases, the metal tricarbonyl fragment stabilizes the nonclassical planar form of the borane rings, whereas the complexes
of metal tricarbonyls based on the classical nonplanar borane conformations are less thermodynamically stable. 相似文献
17.
R. M. Minyaev 《Russian Chemical Bulletin》2012,61(9):1673-1680
Novel stable structures, viz., supertetrahedrane (C104H32), supertetraborane (B104H32), and mixed supertetracarboranes (B64C40H32 and B40C64H32), derived by substituting for carbon atoms in the diamond lattice by tetrahedra C4 and B4, respectively, and being supermolecular models of the corresponding carbon and boron crystalline structures were studied by the DFT B3LYP/6-311+G** method. The low difference in energies of the frontier orbitals indicate semiconduction properties of these compounds. The carbon-carbon, boron-boron, and carbon-boron bonds in the studied compounds are shorter than in diamond and in the borane or carboranes systems, respectively. Along with the calculated vibrational spectra, this indicates that their mechanical properties are similar to those of diamond. However, a considerably low density of these compounds shows their high potential possibility of applying them in aerospace technology. 相似文献
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Wen Cai Huang Hu Zheng Ling Ling Weng 《中国化学快报》2008,19(1):19-22
Tetracycline analogs were designed and synthesized and their bone affinities were tested on hydroxyapatite. The results showed that the carbonyl-amide-enol structure in A ring and phenol-ketone structure in BCD ring may be responsible for tetracycline's high bone affinity and either A ring or BCD ring has a planar conformation is essential. 2007 Ling Ling Weng. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. 相似文献