Search results

Search for "antitumor" in Full Text gives 279 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Stimuli-responsive HBPS-g-PDMAEMA and its application as nanocarrier in loading hydrophobic molecules

  • Yongsheng Chen,
  • Li Wang,
  • Haojie Yu,
  • Zain-Ul-Abdin,
  • Ruoli Sun,
  • Guanghui Jing,
  • Rongbai Tong and
  • Zheng Deng

Beilstein J. Org. Chem. 2016, 12, 939–949, doi:10.3762/bjoc.12.92

Graphical Abstract
  • candidates for transporting hydrophobic guest molecules such as anticancer or antitumor drugs. In the cases of polymeric nanocarriers with responsive shell and stable core, the external hydrophilic shell makes these nanocarriers soluble in water and affords stimuli-responsive properties. The interior
PDF
Album
Full Research Paper
Published 10 May 2016

Indenopyrans – synthesis and photoluminescence properties

  • Andreea Petronela Diac,
  • Ana-Maria Ţepeş,
  • Albert Soran,
  • Ion Grosu,
  • Anamaria Terec,
  • Jean Roncali and
  • Elena Bogdan

Beilstein J. Org. Chem. 2016, 12, 825–834, doi:10.3762/bjoc.12.81

Graphical Abstract
  • ]isochromen-5(11H)-ones have been reported as key intermediates for the development of several topoisomerase I (Top1) anticancer agents [4][5][6][7]. A natural product exhibiting very promising antitumor activity is β-lapachone having a naphtho[1,2-b]pyrandione skeleton [8][9]. Also worth mentioning in this
PDF
Album
Supp Info
Full Research Paper
Published 27 Apr 2016

Synthesis and in vitro cytotoxicity of acetylated 3-fluoro, 4-fluoro and 3,4-difluoro analogs of D-glucosamine and D-galactosamine

  • Štěpán Horník,
  • Lucie Červenková Šťastná,
  • Petra Cuřínová,
  • Jan Sýkora,
  • Kateřina Káňová,
  • Roman Hrstka,
  • Ivana Císařová,
  • Martin Dračínský and
  • Jindřich Karban

Beilstein J. Org. Chem. 2016, 12, 750–759, doi:10.3762/bjoc.12.75

Graphical Abstract
  • galectin-mediated antitumor T cell apoptosis [16]. Some acetylated fluoro hexosamines also displayed antiproliferative properties in vitro [17]. For example, 3- and 4-fluoro-D-glucosamine analogs 5 [18] and 1 [19], and 4-fluoro-D-galactosamine analog 4 [19] (Figure 1), inhibited the growth of murine L1210
PDF
Album
Supp Info
Full Research Paper
Published 20 Apr 2016

Unconventional application of the Mitsunobu reaction: Selective flavonolignan dehydration yielding hydnocarpins

  • Guozheng Huang,
  • Simon Schramm,
  • Jörg Heilmann,
  • David Biedermann,
  • Vladimír Křen and
  • Michael Decker

Beilstein J. Org. Chem. 2016, 12, 662–669, doi:10.3762/bjoc.12.66

Graphical Abstract
  • multiple biological activities and promising therapeutic applications, such as hepatoprotection, antitumor, antiproliferative and anti-oxidant properties [1]. The standardized extract of S. marianum fruits contains the so-called silymarin complex, and is used as the main active component mixture of Legalon
PDF
Album
Supp Info
Full Research Paper
Published 08 Apr 2016

Biosynthesis of α-pyrones

  • Till F. Schäberle

Beilstein J. Org. Chem. 2016, 12, 571–588, doi:10.3762/bjoc.12.56

Graphical Abstract
  • are applied for defense against competitors and predators. The biological activities these compounds exhibit is immense, including antimicrobial [2], antitumor [3][4], and cytotoxic activities [5]. Aflatoxins, produced by several Aspergillus species, are known to cause food poisoning due to their
  • -pyran-2-one (47, Figure 10) [52]. Also antitumor activities of α-pyrones had been shown. Thus, pironetin (47, Figure 10) induced apoptosis in a dose- and time-dependent manner, and tubulin assembly was inhibited in vitro [53]. The natural product was isolated from Streptomyces sp. NK10958 [54], and its
  • monocyclic α-pyrones showing pheromone (47) and antitumor activity (48), respectively. Structures of 6-alkyl (alkoxy or alkylthio)-4-aryl-3-(4-methanesulfonylphenyl)pyrones. Structures of kavalactones. Strutures of germicins. Structures of the pseudopyronines. The structures of the monobenzo-α-pyrone
PDF
Album
Review
Published 24 Mar 2016

Interactions of cyclodextrins and their derivatives with toxic organophosphorus compounds

  • Sophie Letort,
  • Sébastien Balieu,
  • William Erb,
  • Géraldine Gouhier and
  • François Estour

Beilstein J. Org. Chem. 2016, 12, 204–228, doi:10.3762/bjoc.12.23

Graphical Abstract
  • molecules may compromise their activity as poor distribution or passive diffusion across cell membranes are the usual drawbacks associated with their use. Developed after World War II, organophosphorus compounds were used as antitumor [1][2][3][4][5][6][7][8], antiviral [9][10][11][12], antihypertensive [13
PDF
Album
Review
Published 05 Feb 2016

Versatile synthesis and biological evaluation of novel 3’-fluorinated purine nucleosides

  • Hang Ren,
  • Haoyun An,
  • Paul J. Hatala,
  • William C. Stevens Jr,
  • Jingchao Tao and
  • Baicheng He

Beilstein J. Org. Chem. 2015, 11, 2509–2520, doi:10.3762/bjoc.11.272

Graphical Abstract
  • -D-riboside (6-β-D-MPR) is an isolated antibiotic agent that possesses potent antifungal, antiviral, and antitumor activities [44]. In order to explore the effect of fluorine on the biological activity of this pharmacophore, we synthesized 6-methylpurine-3’-deoxy-3’-fluoro-β-D-riboside (4) (Scheme 2
  • riboside 29 exhibited better antitumor activity than its deprotected analog 4, the 3’-fluoro-6-MPR analog. The 6-chlorine compound 22, as well as protected purine nucleosides 32, 39 and 40, also showed potent inhibitory activity. 3’-Fluorine purine nucleosides 2–4, 12, 30, and 49 showed moderate levels of
  • -chloro-intermediates 26 and 48, followed by deprotection, resulted in 6-deaminopurine nucleosides 1 and 21, new analogues of the naturally isolated antibacterial and antineoplastic agent 6-deaminoadenosine, nebularine. Newly synthesized compounds were evaluated for their antitumor activity. Eleven
PDF
Album
Supp Info
Full Research Paper
Published 09 Dec 2015

Recent highlights in biosynthesis research using stable isotopes

  • Jan Rinkel and
  • Jeroen S. Dickschat

Beilstein J. Org. Chem. 2015, 11, 2493–2508, doi:10.3762/bjoc.11.271

Graphical Abstract
  • polyketide products. Emphasizing the same principle, the biosynthesis of trioxacarcin A (9, Scheme 3), a complex aromatic natural product originally isolated from Streptomyces bottropensis DO-45 and showing remarkable antibacterial and antitumor properties [25], was investigated using isotopically labeled
PDF
Album
Review
Published 09 Dec 2015

Syntheses of 2-substituted 1-amino-4-bromoanthraquinones (bromaminic acid analogues) – precursors for dyes and drugs

  • Enas M. Malik,
  • Younis Baqi and
  • Christa E. Müller

Beilstein J. Org. Chem. 2015, 11, 2326–2333, doi:10.3762/bjoc.11.253

Graphical Abstract
  • ][18][19]. AQ derivatives can also exert a variety of pharmacological activities including laxative, anti-inflammatory [20][21], antitumor [22][23], antifungal [24], antiviral [25], and blood platelet inhibitory effects [26][27][28]. Reactive Blue 2 (RB-2), a chlorotriazinyl-containing AQ dye, defined
PDF
Album
Supp Info
Full Research Paper
Published 26 Nov 2015

2-Hetaryl-1,3-tropolones based on five-membered nitrogen heterocycles: synthesis, structure and properties

  • Yury A. Sayapin,
  • Inna O. Tupaeva,
  • Alexandra A. Kolodina,
  • Eugeny A. Gusakov,
  • Vitaly N. Komissarov,
  • Igor V. Dorogan,
  • Nadezhda I. Makarova,
  • Anatoly V. Metelitsa,
  • Valery V. Tkachev,
  • Sergey M. Aldoshin and
  • Vladimir I. Minkin

Beilstein J. Org. Chem. 2015, 11, 2179–2188, doi:10.3762/bjoc.11.236

Graphical Abstract
  • ; Introduction Tropolone derivatives represent one of the promising classes of compounds having a wide spectrum of biological activities: in particular, antitumor activity [1][2], barrier properties with respect to various pathogens, insects and microorganisms [3]. The natural compound hinokitiol (4-isopropyl
PDF
Album
Supp Info
Full Research Paper
Published 12 Nov 2015

A convenient four-component one-pot strategy toward the synthesis of pyrazolo[3,4-d]pyrimidines

  • Mingxing Liu,
  • Jiarong Li,
  • Hongxin Chai,
  • Kai Zhang,
  • Deli Yang,
  • Qi Zhang and
  • Daxin Shi

Beilstein J. Org. Chem. 2015, 11, 2125–2131, doi:10.3762/bjoc.11.229

Graphical Abstract
  • important because of their biological activity [1][2][3][4][5][6]. They have shown a wide range of pharmacological potential such as kinase inhibitors [1], antitumor [7][8], anti-inflammatory [9][10], antimicrobial [11][12][13], pesticides [14], radio protectant [15] and cardiovascular activity [16][17
PDF
Album
Supp Info
Full Research Paper
Published 06 Nov 2015

Stereochemistry of ring-opening/cross metathesis reactions of exo- and endo-7-oxabicyclo[2.2.1]hept-5-ene-2-carbonitriles with allyl alcohol and allyl acetate

  • Piotr Wałejko,
  • Michał Dąbrowski,
  • Lech Szczepaniak,
  • Jacek W. Morzycki and
  • Stanisław Witkowski

Beilstein J. Org. Chem. 2015, 11, 1893–1901, doi:10.3762/bjoc.11.204

Graphical Abstract
  • ., annonaceous acetogenins [3][4], lignans [5][6], iso- and neurofurans [7][8], as well as macrodiolides [9]. These substances exhibit a diverse biological activities including antitumor, antimicrobial, etc. [10][11][12]. Stereoselective construction of substituted tetrahydrofurans is still a challenging task in
PDF
Album
Supp Info
Full Research Paper
Published 13 Oct 2015

An efficient synthesis of N-substituted 3-nitrothiophen-2-amines

  • Sundaravel Vivek Kumar,
  • Shanmugam Muthusubramanian,
  • J. Carlos Menéndez and
  • Subbu Perumal

Beilstein J. Org. Chem. 2015, 11, 1707–1712, doi:10.3762/bjoc.11.185

Graphical Abstract
  • medication for osteoporosis [6] (Figure 1). Other interesting properties identified in 2-aminothiophene derivatives include GluR6 antagonism [7], antiviral and antitumor activities [8][9][10], inhibition of p53-MDM2 interactions [11] and protein-tyrosine phosphatase 1B inhibition [12]. Furthermore, 2
PDF
Album
Supp Info
Full Research Paper
Published 22 Sep 2015

Pyridinoacridine alkaloids of marine origin: NMR and MS spectral data, synthesis, biosynthesis and biological activity

  • Louis P. Sandjo,
  • Victor Kuete and
  • Maique W. Biavatti

Beilstein J. Org. Chem. 2015, 11, 1667–1699, doi:10.3762/bjoc.11.183

Graphical Abstract
  • synthetic compounds, has been widely investigated. Many of them displayed cytotoxic activity in addition to other bioactivities such as antiviral, antifungal, antibacterial, antitumor and antiparasitic potential [41]. Several reviews on pyridoacridine alkaloids have been published between 1983–2015 [35][43
PDF
Album
Review
Published 18 Sep 2015

Structure and conformational analysis of spiroketals from 6-O-methyl-9(E)-hydroxyiminoerythronolide A

  • Ana Čikoš,
  • Irena Ćaleta,
  • Dinko Žiher,
  • Mark B. Vine,
  • Ivaylo J. Elenkov,
  • Marko Dukši,
  • Dubravka Gembarovski,
  • Marina Ilijaš,
  • Snježana Dragojević,
  • Ivica Malnar and
  • Sulejman Alihodžić

Beilstein J. Org. Chem. 2015, 11, 1447–1457, doi:10.3762/bjoc.11.157

Graphical Abstract
  • investigations have shown that beside their antibacterial activity, some macrolides exhibit anti-inflammatory/immunomodulatory [5][6][7][8][9][10], antitumor [11][12][13], antiviral [10] or antimalarial [14][15] activity. These discoveries have sparked a new interest in the structural modification of macrolides
  • sponges, which display extraordinary antitumor activity [29]. At the same time, the spiroketal-containing integramycin acts as an HIV-1 protease inhibitor [27]. The studies of Hayashi et al. have shown that the integrity of the spiroketal subunit is essential for the inhibition of telomerase by
PDF
Album
Supp Info
Full Research Paper
Published 19 Aug 2015

A novel and widespread class of ketosynthase is responsible for the head-to-head condensation of two acyl moieties in bacterial pyrone biosynthesis

  • Darko Kresovic,
  • Florence Schempp,
  • Zakaria Cheikh-Ali and
  • Helge B. Bode

Beilstein J. Org. Chem. 2015, 11, 1412–1417, doi:10.3762/bjoc.11.152

Graphical Abstract
  • sensing; Introduction Chemical compounds containing an α-pyrone moiety are widespread in nature [1][2] and show a high diversity in their biological activity. Members of this class of compounds have been identified with antimicrobial, cytotoxic [3] and antitumor activities [4], as HIV protease inhibitors
PDF
Album
Supp Info
Full Research Paper
Published 12 Aug 2015

Gold-catalyzed formation of pyrrolo- and indolo-oxazin-1-one derivatives: The key structure of some marine natural products

  • Sultan Taskaya,
  • Nurettin Menges and
  • Metin Balci

Beilstein J. Org. Chem. 2015, 11, 897–905, doi:10.3762/bjoc.11.101

Graphical Abstract
  • , such as lukianol A (1) and lukianol B (2) (Figure 1) [8][9][10]. Lukianol B (2) was found to be the most potent human aldose reductase (h-ALR2) inhibitor in thousands of marine natural products screened [11]. The ningalin B alkaloid 3, having an isomeric pyrrolo-oxazinone skeleton, possesses antitumor
PDF
Album
Supp Info
Full Research Paper
Published 28 May 2015

N-Alkyl derivatives of diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside; synthesis and antimicrobial activity

  • Agata Walczewska,
  • Daria Grzywacz,
  • Dorota Bednarczyk,
  • Małgorzata Dawgul,
  • Andrzej Nowacki,
  • Wojciech Kamysz,
  • Beata Liberek and
  • Henryk Myszka

Beilstein J. Org. Chem. 2015, 11, 869–874, doi:10.3762/bjoc.11.97

Graphical Abstract
  • used as detergents, surfactants and emulsifiers. Moreover, they display a wide range of pharmacological activities, including antifungal, antiparasitic, antiinflammatory, antibacterial, and antitumor activities [2][3][4][5]. No wonder, saponins have been evaluated as vaccine adjuvants [6]. Despite the
  • saponins have been investigated [12][13][14][15][16][17][18][19][20][21][22] as well as the evaluation of their antitumor activities [23][24][25][26][27]. Naturally-occurring diosgenyl glycosides are the most abundant steroidal saponins. They have been continuously synthesized [28][29][30][31][32] and
  • demonstrated that diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside hydrochloride increases the number of apoptotic B cells, in combination with cladribine (2-CdA), which were isolated from chronic lymphotic leukemia (B-CLL) patients [40]. The presence of the amine group in this promising antitumor compound
PDF
Album
Supp Info
Full Research Paper
Published 22 May 2015

Exploring monovalent and multivalent peptides for the inhibition of FBP21-tWW

  • Lisa Maria Henning,
  • Sumati Bhatia,
  • Miriam Bertazzon,
  • Michaela Marczynke,
  • Oliver Seitz,
  • Rudolf Volkmer,
  • Rainer Haag and
  • Christian Freund

Beilstein J. Org. Chem. 2015, 11, 701–706, doi:10.3762/bjoc.11.80

Graphical Abstract
  • ]. Aberrant splicing is associated with several diseases [2] and the inhibition of splicing factors has become a recent topic in the field of antitumor drugs [3]. Formin-binding protein 21 (FBP21) has been detected as a component of early spliceosomal complexes and more specifically was shown to interact with
PDF
Album
Supp Info
Letter
Published 11 May 2015

Synthesis of 1,2-cis-2-C-branched aryl-C-glucosides via desulfurization of carbohydrate based hemithioacetals

  • Henok H. Kinfe,
  • Fanuel M. Mebrahtu,
  • Mandlenkosi M. Manana,
  • Kagiso Madumo and
  • Mokela S. Sokamisa

Beilstein J. Org. Chem. 2015, 11, 583–588, doi:10.3762/bjoc.11.64

Graphical Abstract
  • glycochemistry and medicinal chemistry [1][2][3][4][5]. C-Glycosides, especially aryl-C-glycosides, are the main structural features of a number of biologically active natural products such as pluramycins (antibacterial and antitumor activities), angucyclines (antibacterial, antitumor activities, and inhibitors
  • of oxidative enzymes), and benzoisochromanequinones (antibacterial, antitumor and antiplatelet aggregation activities) [2]. Moreover, the stability of the C–C glycosidic bond in C-glycosides provides the potential to serve as inhibitors of carbohydrate degrading enzymes [1][2][3][4][5]. Owing to
PDF
Album
Supp Info
Full Research Paper
Published 29 Apr 2015

The reactions of 2-ethoxymethylidene-3-oxo esters and their analogues with 5-aminotetrazole as a way to novel azaheterocycles

  • Marina V. Goryaeva,
  • Yanina V. Burgart,
  • Marina A. Ezhikova,
  • Mikhail I. Kodess and
  • Viktor I. Saloutin

Beilstein J. Org. Chem. 2015, 11, 385–391, doi:10.3762/bjoc.11.44

Graphical Abstract
  • -oxo esters and their analogues with 5-aminotetrazole (5-AT), although these reactions can be used to generate functionalized tetrazolo[1,5-a]pyrimidines. Derivatives of these heterocycles are promising objects for biological testing, because substances possessing apoptotic and antitumor [13
PDF
Album
Supp Info
Full Research Paper
Published 23 Mar 2015

C-5’-Triazolyl-2’-oxa-3’-aza-4’a-carbanucleosides: Synthesis and biological evaluation

  • Roberto Romeo,
  • Caterina Carnovale,
  • Salvatore V. Giofrè,
  • Maria A. Chiacchio,
  • Adriana Garozzo,
  • Emanuele Amata,
  • Giovanni Romeo and
  • Ugo Chiacchio

Beilstein J. Org. Chem. 2015, 11, 328–334, doi:10.3762/bjoc.11.38

Graphical Abstract
  • by exploiting a click chemistry reaction of 5’-azido-2’-oxa-3’-aza-4’a-carbanucleosides with substituted alkynes. Biological tests indicate an antitumor activity for the synthesized compounds: most of them inhibit cell proliferation of Vero, BS-C-1, HEp-2, MDCK, and HFF cells with a CC50 in the range
  • of 5.0–40 μM. The synthesized compounds do not show any antiviral activity. Keywords: antitumor activity; click chemistry; 1,3-dipolar cycloaddition; nucleic acids; 2’-oxa-3’-aza-4’a-carbanucleoside analogs; Introduction Synthetic modified nucleosides are of great interest as potential new lead
  • -carbanucleoside. However, in order to maintain the six-bond periodicity of the oligonucleotides and thus the flexibility of the oligonucleotide chain the methylene bridge at the pseudo-5’-position was retained. The obtained compounds have shown to be endowed with an interesting antitumor activity: most of them
PDF
Album
Supp Info
Full Research Paper
Published 09 Mar 2015

Copper-catalyzed cascade reactions of α,β-unsaturated esters with keto esters

  • Zhengning Li,
  • Chongnian Wang and
  • Zengchang Li

Beilstein J. Org. Chem. 2015, 11, 213–218, doi:10.3762/bjoc.11.23

Graphical Abstract
  • and its analogues, sharing the similar structure of a γ-lactone with an attached β-carboxylic acid, are widely found in natural products. Related syntheses have been actively explored due to the potential antitumor and antibiotic activities of these compounds [1][2][3][4]. The synthesis methods were
PDF
Album
Supp Info
Full Research Paper
Published 06 Feb 2015

Synthesis and biological evaluation of a novel MUC1 glycopeptide conjugate vaccine candidate comprising a 4’-deoxy-4’-fluoro-Thomsen–Friedenreich epitope

  • Manuel Johannes,
  • Maximilian Reindl,
  • Bastian Gerlitzki,
  • Edgar Schmitt and
  • Anja Hoffmann-Röder

Beilstein J. Org. Chem. 2015, 11, 155–161, doi:10.3762/bjoc.11.15

Graphical Abstract
  • 100-fold diluted antiserum of mouse 2 show fluorescence and appear all in the right area, whereas in the control experiment, cells treated with buffer solution do not show fluorescence and appear in the left area. Conclusion In summary, we have synthesized novel MUC1 antitumor vaccine candidates
PDF
Album
Supp Info
Full Research Paper
Published 23 Jan 2015

Enantioselective synthesis of polyhydroxyindolizidinone and quinolizidinone derivatives from a common precursor

  • Nemai Saha and
  • Shital K. Chattopadhyay

Beilstein J. Org. Chem. 2014, 10, 3104–3110, doi:10.3762/bjoc.10.327

Graphical Abstract
  • , antimetastatic, immunoregulating, antitumor, and anticancer activities [6][7][8][9]. Although naturally occurring polyhydroxylated quinolizidines are less documented, several synthetic derivatives have been prepared in the quest for analogues of the more abundant indolizidines [10][11][12][13][14][15]. Ring-size
PDF
Album
Supp Info
Full Research Paper
Published 22 Dec 2014
Other Beilstein-Institut Open Science Activities