Search results
Search for "anticancer" in Full Text gives 487 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Synthesis and acaricidal activity against Varroa destructor of α- and γ-costic acid dimers
Beilstein J. Org. Chem. 2026, 22, 1088–1096, doi:10.3762/bjoc.22.87
- specific activity has never been reported for γ-costic acid (3), for which only antifeedant [19] and antibacterial activities [8] have been demonstrated. Recently, some of us reported that the synthesized dimeric esters of both polygodial and ophiobolin A with ethylene glycol show enhanced anticancer
- activity with respect to their parent compounds shifting potencies from two-digit to single-digit micromolar levels against apoptosis-resistant cancer cells [20]. Similar increases in anticancer activity have been also reported for dimers of other natural bioactive compounds [20]. Consequently, it was of
Retraction: α,ß-Didehydrosuberoylanilide hydroxamic acid (DDSAHA) as precursor and possible analogue of the anticancer drug SAHA
Beilstein J. Org. Chem. 2026, 22, 1086–1087, doi:10.3762/bjoc.22.86
- Shital K. Chattopadhyay Subhankar Ghosh Sarita Sarkar Kakali Bhadra Department of Chemistry, University of Kalyani, Kalyani - 741235, West Bengal, India Department of Zoology, University of Kalyani, Kalyani - 741235, West Bengal, India 10.3762/bjoc.22.86 Keywords: anticancer drug; cross
One-pot four-component sequential synthesis of S-alkyl dithiocarbamates using lipase as a biocatalyst
Beilstein J. Org. Chem. 2026, 22, 1048–1056, doi:10.3762/bjoc.22.83
- , where they serve as antifungal and anticancer agents. As a result, their synthesis has garnered significant attention in recent years. In this study, we present an efficient one-pot four-component approach for the synthesis of these scaffolds, utilizing aldehydes, ethyl acetoacetate, carbon disulfide
- ]. S-Alkyl dithiocarbamates demonstrate a broad spectrum of bioactivities, including potent anticancer [9], anti-Alzheimer [10][11], antibacterial [12], and antifungal [13][14] properties. In the realm of synthetic organic chemistry, these compounds serve as valuable intermediates, protecting groups
Synthesis of novel 1,2,4-oxadiazole-isoxazoline hybrids and their in silico potential with adenosine receptors
Beilstein J. Org. Chem. 2026, 22, 1033–1047, doi:10.3762/bjoc.22.82
- amide functional groups [1][2][3][4][5]. 1,2,4-Oxadiazole derivatives interact with various receptors as agonists or antagonists, demonstrating a wide spectrum of biological activities including anti-inflammatory, anticancer, antidepressant, anti-HIV, antifungal, and anticonvulsant properties [6][7][8
- developed as pharmacotherapeutic agents so far. Specifically, isoxazoline-based compounds have shown broad biological efficacy, including antimicrobial, anti-inflammatory, anticancer, and antidepressant effects [15][16][17][18][19][20] (Figure 1). Prominent drugs containing isoxazole or isoxazoline rings
Semisynthesis, characterisation, and antibacterial evaluation of a novel lecanoric acid-derived amide library
Beilstein J. Org. Chem. 2026, 22, 1023–1032, doi:10.3762/bjoc.22.81
- investigations. Initial assessment (1H NMR spectroscopy and UHPLC–MS) of the crude CH2Cl2/MeOH extracts of P. tinctorum revealed the presence of a highly abundant natural product previously described as the depside, lecanoric acid (1, Figure 1). Several publications have outlined the antibiotic [3], anticancer
Rh(III)-catalyzed chelation-assisted C–H activation/annulation of 2-arylimidazolines with cyclic diazo-1,3-dicarbonyl compounds: a novel approach to tetracyclic annulated derivatives of 2,3-dihydroimidazo[2,1-a]isoquinoline
Beilstein J. Org. Chem. 2026, 22, 997–1003, doi:10.3762/bjoc.22.78
- many drug candidates and marketed drugs for the treatment of hypertension [2], diabetes [3], and various central nervous system disorders [4]. Recently, imidazolines that exhibit anticancer activity, like nutlins [5][6], have also garnered a lot of interest. There are numerous general methods for
Novel macrocycles: from synthesis to supramolecular function
Beilstein J. Org. Chem. 2026, 22, 982–985, doi:10.3762/bjoc.22.76
- directions for the clinical translation of these materials. Moving from broad biomedical overviews to therapeutic applications, Consoli and co-workers [38] exploit the synthetic versatility of calix[4]arenes to develop selective anticancer systems. By clustering bioactive isothiouronium groups on an
The trans-influence in gold chemistry from a catalytic perspective
Beilstein J. Org. Chem. 2026, 22, 838–856, doi:10.3762/bjoc.22.66
- increased take-up into oestrogen-receptor positive (ER+) breast cancer cells for improved anticancer activity [33]. Similar chelate and pincer gold(III) complexes are potential anticancer therapy targets [34][35][36]. In their assessment of the trans-influence of the C^N^C pincer in comparison with the C^C
Synthesis and structural elucidation of a novel bis-spirooxindole from isatin and ethylenediamine
Beilstein J. Org. Chem. 2026, 22, 813–820, doi:10.3762/bjoc.22.63
- approaches [2][3][4][5]. In this context, comprehensive medicinal chemistry studies consistently highlight the prominence of isatin-derived frameworks among bioactive and anticancer agents [6]. The remarkable reactivity of the isatin scaffold arises from its dual functionality, combining an electrophilic C-3
Preparation of 3-(alkylamino)imidazo[1,2-a]pyridine-2-carbaldehydes via Kornblum oxidation and unexpected ring-opening reactions of the corresponding alcohols under oxidative conditions
Beilstein J. Org. Chem. 2026, 22, 763–770, doi:10.3762/bjoc.22.58
- (4) [4], and HIV (5), [5] to name a few (Figure 1). The imidazo[1,2-a]pyridine drug zolimidine (6) is used for the treatment of gastroesophageal reflux disease [6] while other compounds have exhibited anticancer [7][8] and anti-inflammatory [9][10] activity. More recently, imidazo[1,2-a]pyridine
Anti-invasive and cytotoxic evaluation of a (+)-pinoresinol-based semisynthetic library against glioblastoma
Beilstein J. Org. Chem. 2026, 22, 691–704, doi:10.3762/bjoc.22.54
- anticancer effects [9][10][11][12][13][14]. However, many of the 287 species that make up this genus have not yet been chemically investigated, indicating that Eremophila still has the potential to be the source of new bioactive chemicals and/or known compounds with new biological activity. The use of
- spectrometric techniques. Plants are a vast reservoir of phytochemicals that serve as the source of numerous drugs, including many with anticancer properties [18][19]. These phytochemicals may act on cellular signalling, apoptosis, metabolic pathways, and cell motility in tumor cells. Most anticancer research
- shown to reduce cell invasion in the transwell assay, with an IC50 value of 0.40 µM. These findings provide a rationale for more detailed anticancer studies on pinoresinol and its derivatives in the future. Experimental General experimental procedures Melting points were measured using a Cole-Parmer
Regioselective approach to 5-arylsulfonylisoxazoles and their antimicrobial activity
Beilstein J. Org. Chem. 2026, 22, 592–602, doi:10.3762/bjoc.22.45
- pyridine ring and carboxyl group [6][7][8][9]. On the other hand, the sulfonamide and sulfone groups are commonly found in the design of potential therapeutics with various types of biological activities, such as antimicrobial, antitubercular, antileishmanial, antiviral, anticancer, antidiabetic, anti
Modern synthetic pathways towards eribulin and its subunits
Beilstein J. Org. Chem. 2026, 22, 495–526, doi:10.3762/bjoc.22.37
- described the total synthesis of the marine natural product [19] and shortly thereafter, also its simplified structure, 1, was assembled and showed similar anticancer behavior [19][21]. Since 2010, the mesylate salt of 1 is approved by the U.S. Food and Drug Administration (FDA) for the treatment of
Recent advances in the stereoselective synthesis of distal biaxially chiral molecules
Beilstein J. Org. Chem. 2026, 22, 461–479, doi:10.3762/bjoc.22.34
- distal axial chiralities are widely applied in chiral ligands, natural products, and anticancer agents, with their unique spatial configurations endowing them with distinctive functions and values. Although significant progress has been made in the asymmetric synthesis of distal biaxial chirality
Structural reassignment of compound 968, an allosteric glutaminase inhibitor
Beilstein J. Org. Chem. 2026, 22, 455–460, doi:10.3762/bjoc.22.33
- anticancer drug target. Compound 968 is a glutaminase inhibitor that is widely used to probe cancer cells’ dependence on glutaminase activity. Here, we show by NMR spectroscopy and X-ray crystallography that the reported benzo[c]phenanthridine structure of compound 968 is incorrect; its true structure is the
- demands of the proliferative state creates an opportunity to selectively target cancer cells [1][7]. Chemical inhibition of GLS has emerged as an attractive anticancer strategy, and several classes of GLS inhibitors have been discovered [1][2]. DON is a diazo-containing electrophilic glutamine analog that
- and stabilizes a catalytically inactive form of the enzyme [11][12]. The BPTES scaffold has undergone significant medicinal chemistry development resulting in CB-839/telaglenastat, which is being evaluated in clinical trials in combination with other anticancer agents [13]. Compound 968 is a third
Synthesis and anti-cancer activity of naphthalimide–organylselanyl conjugates
Beilstein J. Org. Chem. 2026, 22, 416–435, doi:10.3762/bjoc.22.29
- optimisation. In this study, we report the in-silico modelling and anticancer activity of two 1,8-napthalimide (NAP) derivatives containing organyl selanyl groups. The organylselanyl function n-octylselanyl (n-OctSe) or phenylselanyl (PhSe) was introduced at the 6-position of a naphthalimide structure having a
- structurally characterised by single-crystal X-ray diffraction analysis. The anticancer potential of the NAP-SePh and NAP-Se(n-Oct) was evaluated using an in vitro cell viability assay with MDA-MB-231 triple-negative breast cancer (TNBC) cells. The IC₅₀ values for compounds NAP-SePh and NAP-Se(n-Oct) were
- epidermal growth factor receptor (EGFR) in which erlotinib, a well-known anticancer drug, binds. Keywords: cell line study; density functional theory; MDA-MB-231; molecular docking; organoselanyl conjugates; Introduction Cancer remains one of the most common and life-threatening diseases globally, posing
Design, synthesis and biological evaluation of 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines as selective cytotoxic agents against HeLa cells
Beilstein J. Org. Chem. 2026, 22, 390–398, doi:10.3762/bjoc.22.27
- liquid chromatography–mass spectrometry. Their anticancer activity was assessed against human cancer cell as well as non-cancer cell lines. Three compounds, 1, 3, and 9, were the most cytotoxic to HeLa cells (IC50 = 6.13 ± 1.95, 13.99 ± 1.80 and 49.92 ± 3.98 μM, respectively). However, only compounds 1
- , 7, and 9 were selective against the tested lines. Compound 9 can be classified as the most attractive and promising candidate for further development against cervical adenocarcinoma. Keywords: ADMET analysis; anticancer activity; 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines; Introduction Purine
- -mimicking scaffolds are a proven strategy in the design of anticancer drugs. Many cancer-related proteins (e.g., kinases, ATPases, DNA/RNA polymerases) have binding pockets designed for purine nucleotides (ATP, GTP). Oxazolopyrimidines can compete with purines or their analogues, inhibiting enzymatic
Spirobarbiturates with a pyrrolizidine moiety: synthesis, structure and biological evaluation
Beilstein J. Org. Chem. 2026, 22, 274–288, doi:10.3762/bjoc.22.20
- animals [31][32][33]. However, some representatives of these compounds (Scheme 2) find applications in pharmacology [34] due to their antimicrobial (megalanthonine; subulacine N-oxide) [35][36], anti-inflammatory (lindelofidine, benzoic acid ester; paludosine) [37][38], anticancer (ligulachyroine) [39
Total synthesis of natural products based on hydrogenation of aromatic rings
Beilstein J. Org. Chem. 2026, 22, 88–122, doi:10.3762/bjoc.22.4
- sustained interest from synthetic chemists worldwide due to their pronounced antibacterial and anticancer properties. Since their discovery, bis-THIQ scaffolds have been constructed primarily through the Pictet–Spengler reaction, a cyclization strategy that continues to be widely employed in total synthesis
Total synthesis of asperdinones B, C, D, E and terezine D
Beilstein J. Org. Chem. 2025, 21, 2730–2738, doi:10.3762/bjoc.21.210
- indole alkaloids is known for its biomedical importance [2]. These alkaloids have been isolated from plants [3], marine sources [4], bacterial sources [5][6][7], and they are particularly relevant primarily because of their potent pharmacological activities as among other, anticancer drugs, but also for
Competitive cyclization of ethyl trifluoroacetoacetate and methyl ketones with 1,3-diamino-2-propanol into hydrogenated oxazolo- and pyrimido-condensed pyridones
Beilstein J. Org. Chem. 2025, 21, 2716–2729, doi:10.3762/bjoc.21.209
- ], fluopyram [36], and the nematicide fluazaindolisine [37] (Figure 1). The trifluoromethyl piperidine backbone is part of the structure of anticancer [38] and antirheumatic [39] agents. The fluorine-containing pyridines and their heteroannelated derivatives are known to exhibit a high biological potential, on
Thiazolidinones: novel insights from microwave synthesis, computational studies, and potentially bioactive hybrids
Beilstein J. Org. Chem. 2025, 21, 2618–2636, doi:10.3762/bjoc.21.203
- , ciglitazone, and rosiglitazone [9][10]. Rhodanine (2-thioxothiazolidin-4-one) derivatives exhibit a wide range of pharmacological activities, including antiviral [11], antimalarial [12], antimicrobial [13], anti-inflammatory [14], anticancer [15], antidiabetic [16], antibacterial [17], and antifungal [18
Synthesis and characterization of a isothiouronium-calix[4]arene derivative: self-assembly and anticancer activity
Beilstein J. Org. Chem. 2025, 21, 2535–2541, doi:10.3762/bjoc.21.195
- , and low toxicity make calixarene derivatives valuable drug candidates against cancer. The aim of the present study was the synthesis and characterization of a calix[4]arene derivative in which known anticancer isothiouronium groups were clustered on a calix[4]arene scaffold bearing long C12 alkyl
- confirmed by comparison with the calix[4]arene precursor (1) lacking these functional units. The selective antiproliferative profile of compound 3 highlights its potential as a lead anticancer agent. Moreover, compound 3 holds promise for further development in combination multidrug therapy due to the
- potential to load drug molecules in the bioactive nanoassembled structure. Keywords: anticancer agent; calixarene; nanostructure; self-assembly; Introduction Cancer remains one of the leading causes of morbidity and mortality worldwide. Despite significant advancements in chemotherapy, more effective and
Pentacyclic aromatic heterocycles from Pd-catalyzed annulation of 1,5-diaryl-1,2,3-triazoles
Beilstein J. Org. Chem. 2025, 21, 2524–2534, doi:10.3762/bjoc.21.194
- ][21], and materials [22][23][24]. Numerous examples of 1,4-diaryl-1,2,3-triazoles with quinoline and isoquinoline subunits have been reported, including those with anticancer [25][26][27][28][29], antiviral [30][31], antibacterial [32], antifungal [33], antimalarial [34][35], antitubercular [36], and
Halogenated butyrolactones from the biomass-derived synthon levoglucosenone
Beilstein J. Org. Chem. 2025, 21, 2297–2301, doi:10.3762/bjoc.21.175
- dichloro-magnesium enolates to protected ᴅ-glyceraldehyde [11]. In 1988, Hertel et al. from the Lilly laboratories published the first synthesis of the clinically important anticancer agent gemcitabine, using an intermediate γ-butyrolactone constructed using protected ᴅ-glyceraldehyde and ethyl
Other Beilstein-Institut Open Science Activities
