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Search for "cancer" in Full Text gives 493 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Phenolic constituents from twigs of Aleurites fordii and their biological activities

  • Kyoung Jin Park,
  • Won Se Suh,
  • Da Hye Yoon,
  • Chung Sub Kim,
  • Sun Yeou Kim and
  • Kang Ro Lee

Beilstein J. Org. Chem. 2021, 17, 2329–2339, doi:10.3762/bjoc.17.151

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  • , respectively, only compound 8 showed a significant activity (96.2 ± 1.1% for 3). The other compounds exhibited moderate or no NGF secretion effect. The cytotoxicity of compounds 1–19 was also evaluated against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) through an SRB assay. All the
  • were expressed as a percentage of the control group (untreated cells). Cytotoxicity assessment. The SRB assay was performed to evaluate cytotoxicity of all the isolated compounds against four cultured human cancer cell lines. The cell lines (National Cancer Institute, Bethesda, MD, USA) were used A549
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Published 07 Sep 2021

Post-functionalization of drug-loaded nanoparticles prepared by polymerization-induced self-assembly (PISA) with mitochondria targeting ligands

  • Janina-Miriam Noy,
  • Fan Chen and
  • Martina Stenzel

Beilstein J. Org. Chem. 2021, 17, 2302–2314, doi:10.3762/bjoc.17.148

Graphical Abstract
  • increase activity [11][12]. These nanoparticles have been decorated with targeting ligands to enhance the accumulation of the drug in cancer tissue. The activity of arsenic drugs could, however, also be enhanced by targeting mitochondria inside the cells, the target of action of arsenic drugs. To the
  • cellular internalization as well as accumulation at the diseased tissues by targeting specific over-expressed receptors in cancer cells. However, to this date it is still debateable if active retention truly causes this "homing" effect. It has been shown that due to increased protein corona formation on a
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Published 03 Sep 2021

(Phenylamino)pyrimidine-1,2,3-triazole derivatives as analogs of imatinib: searching for novel compounds against chronic myeloid leukemia

  • Luiz Claudio Ferreira Pimentel,
  • Lucas Villas Boas Hoelz,
  • Henayle Fernandes Canzian,
  • Frederico Silva Castelo Branco,
  • Andressa Paula de Oliveira,
  • Vinicius Rangel Campos,
  • Floriano Paes Silva Júnior,
  • Rafael Ferreira Dantas,
  • Jackson Antônio Lamounier Camargos Resende,
  • Anna Claudia Cunha,
  • Nubia Boechat and
  • Mônica Macedo Bastos

Beilstein J. Org. Chem. 2021, 17, 2260–2269, doi:10.3762/bjoc.17.144

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  • through isosterism (classical or non-classical) in the design of new active compounds has shown good results [22][23]. Specifically, in the development of new inhibitors for the treatment of cancer [24], its use is associated with producing compounds able to overcoming resistance (primary or secondary
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Published 01 Sep 2021

Constrained thermoresponsive polymers – new insights into fundamentals and applications

  • Patricia Flemming,
  • Alexander S. Münch,
  • Andreas Fery and
  • Petra Uhlmann

Beilstein J. Org. Chem. 2021, 17, 2123–2163, doi:10.3762/bjoc.17.138

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Published 20 Aug 2021

Catalyzed and uncatalyzed procedures for the syntheses of isomeric covalent multi-indolyl hetero non-metallides: an account

  • Ranadeep Talukdar

Beilstein J. Org. Chem. 2021, 17, 2102–2122, doi:10.3762/bjoc.17.137

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  • hydride will become exceptionally crucial when its hydrogen atoms are replaced by this special heterocycle, forming a multi-indolyl hetero non-metallide. In contemporary period, the said molecules have earned extensive importance in pharmacology to prevent cancer of a number of human organs, certified by
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Published 19 Aug 2021

On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets

  • Renato L. Carvalho,
  • Amanda S. de Miranda,
  • Mateus P. Nunes,
  • Roberto S. Gomes,
  • Guilherme A. M. Jardim and
  • Eufrânio N. da Silva Júnior

Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126

Graphical Abstract
  • against different types of diseases, such as cancer [1][2], malaria [3][4], Chagas disease [5][6], HIV [7][8], depression [9][10], amnesia [11], Alzheimer [12], and maybe even in a more recent scenario, COVID-19 [13]. Even though many compounds are found to present activity against these diseases, only a
  • oxonium species in the methylation step. Abiraterone acetate (53) is a drug used in cancer treatment [138]. The Mn-catalyzed methylation of an abiraterone analogue was achieved by replacing the fluorination step by mesylation in 15% of overall yield and only a single diastereoisomer was observed (Scheme
  • was demonstrated by the synthesis of bioactive compounds like an IRAP inhibitor (104) and an antibreast cancer agent (105) in good yields (Scheme 34D). Iron is by far the cheapest and most abundant metal to be used from the 3d series, and these facts are reflected by the amount and quality of studies
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Published 30 Jul 2021

Natural products in the predatory defence of the filamentous fungal pathogen Aspergillus fumigatus

  • Jana M. Boysen,
  • Nauman Saeed and
  • Falk Hillmann

Beilstein J. Org. Chem. 2021, 17, 1814–1827, doi:10.3762/bjoc.17.124

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  • breast cancer cells by arresting the cell cycle and promoting apoptosis while showing no cytotoxicity against RAW 264.7 cells, thus demonstrating their selectivity [65][67]. Further, fumigaclavine was shown to exhibit antibacterial properties and to contribute to virulence in the model insect Galleria
  • [72]. It was further shown to be cytotoxic and inhibiting cell cycle progression at G2/M phase [163]. Fumitremorgin C was shown to effect mammalian cells and inhibit the breast cancer resistance protein which imparts multidrug resistance and thus resistance to chemotherapeutics in breast cancer
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Published 28 Jul 2021

A systems-based framework to computationally describe putative transcription factors and signaling pathways regulating glycan biosynthesis

  • Theodore Groth,
  • Rudiyanto Gunawan and
  • Sriram Neelamegham

Beilstein J. Org. Chem. 2021, 17, 1712–1724, doi:10.3762/bjoc.17.119

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  • pathways is largely unknown. In this work, we performed data mining of TF–glycogene relationships from the Cistrome Cancer database (DB), which integrates chromatin immunoprecipitation sequencing (ChIP-Seq) and RNA-Seq data to constitute regulatory relationships. In total, we observed 22,654 potentially
  • significant TF–glycogene relationships, which include interactions involving 526 unique TFs and 341 glycogenes that span 29 the Cancer Genome Atlas (TCGA) cancer types. Here, TF–glycogene interactions appeared in clusters or so-called communities, suggesting that changes in single TF expression during both
  • relate cell-signaling pathways to TFs and cellular glycosylation state. Whereas analysis results are presented for all 29 cancer types, specific focus is placed on human luminal and basal breast cancer disease progression. Overall, the article presents a computational approach to describe TF–glycogene
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Published 22 Jul 2021

Chemical approaches to discover the full potential of peptide nucleic acids in biomedical applications

  • Nikita Brodyagin,
  • Martins Katkevics,
  • Venubabu Kotikam,
  • Christopher A. Ryan and
  • Eriks Rozners

Beilstein J. Org. Chem. 2021, 17, 1641–1688, doi:10.3762/bjoc.17.116

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  • enabled uptake of the conjugate in DU145 cancer cells as analyzed by fluorescence-activated cell sorting (FACS). However, the conjugate did not inhibit the targeted human telomerase in cells [170]. Langel and co-workers conjugated antisense PNA targeting mRNA of galanin receptor type 1 (GalR1) through
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Published 19 Jul 2021

Recent advances in the application of isoindigo derivatives in materials chemistry

  • Andrei V. Bogdanov and
  • Vladimir F. Mironov

Beilstein J. Org. Chem. 2021, 17, 1533–1564, doi:10.3762/bjoc.17.111

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  • photoelectrochemical reduction of water, as matrix for MALDI spectrometry and in photothermal cancer therapy are also shown. Data published over the past 5 years, including works published at the beginning of 2021, are given. Keywords: isoindigo; OFET; photoactive polymers; photovoltaics; solar cells; Introduction
  • existing polymer conductive binder mixed with carbon additives (Scheme 31). Isoindigo derivatives have begun to find use in biomedical applications. Thus, nanoparticles of isoindigoid polymers have shown good potential as agents for photoacoustic and photothermal cancer therapy [116][117][118][119][120
  • [120]. At the same time, in vivo experiments have shown the high efficiency of low-molecular-weight isoindigo 71 in oxygen sensitization for cancer therapy [121]. Therein, a high value (84%) of the singlet oxygen quantum yield was obtained. Conclusion To summarize, it can be concluded that isoindigo is
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Published 06 Jul 2021

Iodine-catalyzed electrophilic substitution of indoles: Synthesis of (un)symmetrical diindolylmethanes with a quaternary carbon center

  • Thanigaimalai Pillaiyar,
  • Masoud Sedaghati,
  • Andhika B. Mahardhika,
  • Lukas L. Wendt and
  • Christa E. Müller

Beilstein J. Org. Chem. 2021, 17, 1464–1475, doi:10.3762/bjoc.17.102

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  • biological activities (Figure 1) [10]. Unsubstituted DIM (I), for example, exhibits antimicrobial [5], anticancer [11][12][13], and anti-inflammatory effects (Figure 1) [14]. There is preclinical evidence for activity against several types of cancer [15], and DIM has been clinically evaluated for the
  • treatment of prostate cancer [16] and showed promise for the treatment of cervical dysplasia [17]. The related trisindoline (II) was reported to possess antibiotic activity [18], while DIM derivatives III and IV also showed anticancer activities (Figure 1). Owing to their exciting biological activities, DIM
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Published 18 Jun 2021

Synthesis of 1-indolyl-3,5,8-substituted γ-carbolines: one-pot solvent-free protocol and biological evaluation

  • Premansh Dudhe,
  • Mena Asha Krishnan,
  • Kratika Yadav,
  • Diptendu Roy,
  • Krishnan Venkatasubbaiah,
  • Biswarup Pathak and
  • Venkatesh Chelvam

Beilstein J. Org. Chem. 2021, 17, 1453–1463, doi:10.3762/bjoc.17.101

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  • cancer cells. Keywords: γ-carboline; cascade reaction; cell uptake; cytotoxicity; fluorescence; Introduction Carbolines are privileged aza-heterocycles found in the core of several natural and synthetic compounds and are known for their biological applications. Among the four different isomers, 9H
  • effective against cervical cancer (HeLa cells) [8]. Moreover, γ-carbolines are known for their well-established DNA intercalating [9] and anti-Alzheimer [10] properties. The classical Graebe–Ullmann synthesis [11] of γ-carbolines, one of the very early protocols in the domain, is based on the thermal
  • with a standard drug, doxorubicin, were screened for their cytotoxicity against various cancer lines (Figure 5, Table 3 and Figure S2, in Supporting Information File 1) such as MCF-7 (breast cancer), HeLa (cervical cancer), HEK293 (human embryonic kidney cells), A431 (skin cancer), A549 (lung cancer
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Published 17 Jun 2021

Analogs of the carotane antibiotic fulvoferruginin from submerged cultures of a Thai Marasmius sp.

  • Birthe Sandargo,
  • Leon Kaysan,
  • Rémy B. Teponno,
  • Christian Richter,
  • Benjarong Thongbai,
  • Frank Surup and
  • Marc Stadler

Beilstein J. Org. Chem. 2021, 17, 1385–1391, doi:10.3762/bjoc.17.97

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  • cytotoxicity was assessed in vitro against mouse fibroblast cell line L929, cervix carcinoma cell line KB3.1, ovarian cancer cell line SKOV-3, human adenocarcinoma cell lines MCF-7 and PC-3, and human epidermoid carcinoma cell line A431, using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium
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Published 04 Jun 2021

N-tert-Butanesulfinyl imines in the asymmetric synthesis of nitrogen-containing heterocycles

  • Joseane A. Mendes,
  • Paulo R. R. Costa,
  • Miguel Yus,
  • Francisco Foubelo and
  • Camilla D. Buarque

Beilstein J. Org. Chem. 2021, 17, 1096–1140, doi:10.3762/bjoc.17.86

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Published 12 May 2021

Synthetic accesses to biguanide compounds

  • Oleksandr Grytsai,
  • Cyril Ronco and
  • Rachid Benhida

Beilstein J. Org. Chem. 2021, 17, 1001–1040, doi:10.3762/bjoc.17.82

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  • pancreatic carcinoma and triple-negative breast cancer (Scheme 23B) [55]. Konteatis et al. adopted a similar approach by using the direct fusion for the preparation of bisdifluorocyclic biguanides as IDH1/2 inhibitor intermediates (Scheme 23C) [56]. However, sodium dicyanamide has been mainly used as an
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Published 05 May 2021

Synthesis of 10-O-aryl-substituted berberine derivatives by Chan–Evans–Lam coupling and investigation of their DNA-binding properties

  • Peter Jonas Wickhorst,
  • Mathilda Blachnik,
  • Denisa Lagumdzija and
  • Heiko Ihmels

Beilstein J. Org. Chem. 2021, 17, 991–1000, doi:10.3762/bjoc.17.81

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  • , it has been found that berberine (1a) exhibits a selective cytotoxicity against cancer cells [12][13], which is mainly based on its DNA-binding properties [14]. Since the complexation with DNA leads to significant changes of the fluorescent quantum yields of the bound berberine, it can also be used
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Published 04 May 2021

Stereoselective synthesis and transformation of pinane-based 2-amino-1,3-diols

  • Ákos Bajtel,
  • Mounir Raji,
  • Matti Haukka,
  • Ferenc Fülöp and
  • Zsolt Szakonyi

Beilstein J. Org. Chem. 2021, 17, 983–990, doi:10.3762/bjoc.17.80

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  • very good agonist for the S1P1 receptor (Figure 1). Sphingosine 1-phosphate (S1P, 4), in turn, performed critical regulator functions in many physiological and pathological treatments, such as Alzheimer’s disease [8][9], cancer [10][11][12][13], multiple sclerosis [14], and inflammation [15]. Due to
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Published 03 May 2021

Application of the Meerwein reaction of 1,4-benzoquinone to a metal-free synthesis of benzofuropyridine analogues

  • Rashmi Singh,
  • Tomas Horsten,
  • Rashmi Prakash,
  • Swapan Dey and
  • Wim Dehaen

Beilstein J. Org. Chem. 2021, 17, 977–982, doi:10.3762/bjoc.17.79

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  • cancer cell lines [12][13]. Fluoroquinophenoxazines 2 have been used as telomerase inhibitors in anticancer research [14]. Furthermore, benzofuroisoindoles 3 were part of a kinase inhibitor study [15]. Photobiologically active psoralene (linear furocoumarin) dibenzofurans 1 and angular furanocoumarin
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Published 30 Apr 2021

Beyond ribose and phosphate: Selected nucleic acid modifications for structure–function investigations and therapeutic applications

  • Christopher Liczner,
  • Kieran Duke,
  • Gabrielle Juneau,
  • Martin Egli and
  • Christopher J. Wilds

Beilstein J. Org. Chem. 2021, 17, 908–931, doi:10.3762/bjoc.17.76

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  • overall steps [164]. ASOs containing these modified nucleosides have demonstrated promising antitumor activity for lymphoma and lung cancer [165]. Numerous other LNA analogues have been constructed including, but not limited to, 2'-N-guanidino,4'-C-ethylene (GENA) (Figure 7I) [166], sulfonamide-bridged
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Published 28 Apr 2021

Enhanced target cell specificity and uptake of lipid nanoparticles using RNA aptamers and peptides

  • Roslyn M. Ray,
  • Anders Højgaard Hansen,
  • Maria Taskova,
  • Bernhard Jandl,
  • Jonas Hansen,
  • Citra Soemardy,
  • Kevin V. Morris and
  • Kira Astakhova

Beilstein J. Org. Chem. 2021, 17, 891–907, doi:10.3762/bjoc.17.75

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  • –maleimide–PEG into their LNPs to target epidermal growth factor receptor (EGFR)-positive cancer cells. The authors showed an increased delivery of siRNAs and fluorescent quantum dot nanocrystals both in vitro and in EGFR-positive tumor xenografts in mice [48]. In 2020, Chandra et al. used a maleimide–PEG in
  • their LNP formulation to functionalize LNPs with an aptamer specific for the human epidermal growth factor 2 (HER2) receptor. Therein, functionalized LNPs increased siRNA delivery and subsequent sensitivity of the doxorubicin-resistant HER2-positive breast cancer cell lines by ≈2-fold over LNPs with no
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Published 26 Apr 2021

Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects

  • Shivani Gulati,
  • Stephy Elza John and
  • Nagula Shankaraiah

Beilstein J. Org. Chem. 2021, 17, 819–865, doi:10.3762/bjoc.17.71

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  • longer reaction time (3 h) with lower yields (60%) as compared to microwave (20 min with 91% yield). The library of molecules synthesized was found to be active against SKOV-3 cancer cells with 9a emerging as a promising molecule with IC50 = 0.24 ± 0.05 μM (Scheme 3). The protocol surfaces the efficiency
  • subjecting them to the potential dipolarophile but-2-ynedionates to deliver the target molecules. Both the reactions proceeded well in water aiding in greener synthesis of biologically active molecules. The synthesized molecules exhibited significant activity against human lung cancer cell line A549. A
  • cancer cell lines along with good antimicrobial activity (Scheme 24). The proposed mechanism (Scheme 25) involved a Knoevenagel condensation between aldehyde 5 and malononitrile (51) to form arylidene intermediate A. Then A reacts with isocyanide 21 to produce intermediate B which coordinates with 1,10
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Published 19 Apr 2021

DNA with zwitterionic and negatively charged phosphate modifications: Formation of DNA triplexes, duplexes and cell uptake studies

  • Yongdong Su,
  • Maitsetseg Bayarjargal,
  • Tracy K. Hale and
  • Vyacheslav V. Filichev

Beilstein J. Org. Chem. 2021, 17, 749–761, doi:10.3762/bjoc.17.65

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  • +{FAM} ON and it was only present in the cytoplasm. These results indicate that ONs with phosphate modifications such as N+ or Ts might be suitable tools for the application of DNA and RNA vaccines [60], for the treatment of cancer [61], infectious diseases [62], and neurological disorders [63
  • . Maksim V. Kvach for valuable discussions and suggestions. We also thank Mr. Raoul Solomon for assistance in the preparation of Figure 3 and Figure 4. Funding V.V.F. and Y.S. are grateful for the financial support provided by the School of Fundamental Sciences (Massey University) and Cancer Society of New
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Published 29 Mar 2021

Simulating the enzymes of ganglioside biosynthesis with Glycologue

  • Andrew G. McDonald and
  • Gavin P. Davey

Beilstein J. Org. Chem. 2021, 17, 739–748, doi:10.3762/bjoc.17.64

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  • ganglioside biosynthesis, and altered ganglioside status in cancer, and the effects on network structure are predicted. The simulator is available at the Glycologue website, https://glycologue.org/. Keywords: gangliosides; Glycologue; glycosyltransferases; neuropathy; Svennerholm nomenclature; Introduction
  • disorders of ganglioside biosynthesis can lead to a number of neuropathies, including motor deficits, microcephaly, sensory loss, and autistic features [10][11]. Certain gangliosides, such as GM2, have been identified as tumor markers for breast cancer stem cells [12], while members of the alpha-series
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Published 23 Mar 2021

Amino- and polyaminophthalazin-1(2H)-ones: synthesis, coordination properties, and biological activity

  • Zbigniew Malinowski,
  • Emilia Fornal,
  • Agata Sumara,
  • Renata Kontek,
  • Karol Bukowski,
  • Beata Pasternak,
  • Dariusz Sroczyński,
  • Joachim Kusz,
  • Magdalena Małecka and
  • Monika Nowak

Beilstein J. Org. Chem. 2021, 17, 558–568, doi:10.3762/bjoc.17.50

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  • production [11] that plays an important role in the growth of various cancerous tissues (colon, lung, and breast cancer) and as antagonists of the human A3 adenosine receptor [12]. Aminophthalazines have been also evaluated for their inhibitory activity toward phosphodiesterases such as PDE-5 (Figure 1) [13
  • cytotoxicity, proliferation and growth of HT-29 (human colon adenocarcinoma cell line), PC-3 (human prostate cancer cell line) and L-929 cells (mouse fibroblast cell line). The results obtained from the MTT assay revealed that the tested phthalazinone derivatives were cytotoxic towards the tested cell lines in
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Published 25 Feb 2021
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  • a low (1 mol %) catalyst loading, to obtain enantiomerically enriched β-naphthyl-β-sulfanyl ketones with up to 96% ee. The target adducts are the core structure of seco-raloxifene derivatives, which are potent anti-breast cancer agents [32]. In addition, the same scaffold has also shown urease
  • , which have potent activity against breast cancer. The easy access to the corresponding sulfones presents a versatile route for the implementation of a new biologically active moiety, the sulfone, to the β-naphthyl-β-sulfanyl ketones. The enantioenriched products of both classes can be evaluated as
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Published 18 Feb 2021
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