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Search for "anticancer" in Full Text gives 441 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Synthesis, structure, ionochromic and cytotoxic properties of new 2-(indolin-2-yl)-1,3-tropolones
Beilstein J. Org. Chem. 2025, 21, 358–368, doi:10.3762/bjoc.21.26
- [16][17]. Indole derivatives, including those with conjugated aromatic and alicyclic rings, are of considerable interest because of their diverse biological activities (antibacterial, antimicrobial, anticancer, antidiabetic, etc.) [18][19][20][21][22]. For this reason, the synthetic goal of this work
- MTT assay was used to determine the anticancer activity of compound 7a against these cultures (Figure 6). The viability test is an important method to determine which new compounds are able to target cancer cells. The results of this test (IC50 value ± 95% confidence interval) allow us to evaluate the
- possibility of carrying out subsequent stages of research and selecting promising compounds for the further development of anticancer drugs [30]. The study showed that the IC50 inhibitory concentration of 2-(1,1-dimethyl-1H-benzo[e]indolin-2-yl)-5,6,7-trichloro-1,3-tropolone (7a) against the A431 skin cancer
Synthesis, characterization, antimicrobial, cytotoxic and carbonic anhydrase inhibition activities of multifunctional pyrazolo-1,2-benzothiazine acetamides
Beilstein J. Org. Chem. 2025, 21, 348–357, doi:10.3762/bjoc.21.25
- assays [36] (Figure 1A). In continuation of this work, these derivatives have also been investigated for their remarkable anti-HIV-1 activity [37] (Figure 1B). The same research group reported the synthesis of acetamide derivatives of pyrazolo-1,2-benzothiazines as anticancer drugs using a borane-THF
Synthesis of new condensed naphthoquinone, pyran and pyrimidine furancarboxylates
Beilstein J. Org. Chem. 2025, 21, 340–347, doi:10.3762/bjoc.21.24
- heterocyclic structures leads to the production of new types of heterocyclic compounds with practical useful properties [1][2][3][4][5][6]. Representatives of the naphthofuran series exhibit anticancer [7] and antiinfectious activity [8]. Anticancer properties have also been found in representatives of the
Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus Samsoniella aurantia
Beilstein J. Org. Chem. 2025, 21, 327–339, doi:10.3762/bjoc.21.23
- anticancer properties [6]. With concerns about biofilm formation and resistance escalating in the medical field, entomopathogenic fungi have emerged as a promising source of novel bioactive compounds [5]. Our recent exploration of B. neobassiana highlighted this growing interest, affording one tetramic acid
Dioxazolones as electrophilic amide sources in copper-catalyzed and -mediated transformations
Beilstein J. Org. Chem. 2025, 21, 200–216, doi:10.3762/bjoc.21.12
- secondary amines via an N-acyl nitrene intermediate [77]. Amidines, found in biologically active compounds, have been widely investigated in medicinal chemistry due to their potent antiviral, antibacterial, anticancer, and other therapeutic properties [78][79][80][81]. As shown in Scheme 4, dioxazolones
Non-covalent organocatalyzed enantioselective cyclization reactions of α,β-unsaturated imines
Beilstein J. Org. Chem. 2024, 20, 3221–3255, doi:10.3762/bjoc.20.268
- that some of the derivatives exhibit strong anticancer activity against Hela and MCF-7 cell lines. In early 2021, Mei, Lu and co-worker reported a chiral phosphoric acid-catalyzed asymmetric [4 + 2] cycloaddition of aurone-derived 1-azadienes 11 and 3-vinylindoles 61 (Scheme 23). This methodology
Ceratinadin G, a new psammaplysin derivative possessing a cyano group from a sponge of the genus Pseudoceratina
Beilstein J. Org. Chem. 2024, 20, 3215–3220, doi:10.3762/bjoc.20.267
- derivatives exhibit a range of bioactivities, including antibacterial, anticancer, antimalarial, and antiviral effects. Since the discovery of the first psammaplysin derivative, psammaplysin A [4][5], these alkaloids have been recognized as challenging targets for total synthesis. The absolute configuration
Hypervalent iodine-mediated intramolecular alkene halocyclisation
Beilstein J. Org. Chem. 2024, 20, 3113–3133, doi:10.3762/bjoc.20.258
- cost effective and selective, one-pot transformation. Pharmaceutical uses for bio-active cyclic molecules accessible by I(III) reagents are plentiful; anticancer drugs can be formed from the basis of pyrrolo[2,3-b]indoles 1 [3][4], 2-oxazolines 2 [5][6], dihydrofuran 3 [7][8], and spirocyclic scaffolds
Advances in the use of metal-free tetrapyrrolic macrocycles as catalysts
Beilstein J. Org. Chem. 2024, 20, 3085–3112, doi:10.3762/bjoc.20.257
- applied in various fields, including organometallic catalysis, dye-sensitized solar cells, sensing, artificial olfactory systems, photodynamic therapy (PDT), anticancer drugs, biochemical probes, and electrochemical devices. Relevant examples of these two pyrrolic macrocycles as metal-free organocatalysts
Synthesis of the 1,5-disubstituted tetrazole-methanesulfonylindole hybrid system via high-order multicomponent reaction
Beilstein J. Org. Chem. 2024, 20, 3077–3084, doi:10.3762/bjoc.20.256
- representative studies include antibacterial, anti-inflammatory, antioxidant, selective inhibitor of COX-2 [34], and anti-HIV activity [35]. In this context, even though indole is considered a privileged scaffold present in some anticancer agents [36], a few examples of methanesulfonylindoles are studied as
- potential in anticancer drug design. However, it should be taken into account that the sulfonyl group can radically change the pharmacokinetic properties of a drug, so the effect it may have on its ADMET properties should be determined in an additional study. Conclusion A novel synthetic strategy has been
Chemical structure metagenomics of microbial natural products: surveying nonribosomal peptides and beyond
Beilstein J. Org. Chem. 2024, 20, 3050–3060, doi:10.3762/bjoc.20.253
- molecules were screened for various bioactivities and led to the discovery of new antibiotics, antifungals, as well as anticancer compounds (Figure 4). Importantly, the underlying mechanism of bacterial growth suppression has been identified for several Syn-BNP antibiotics, which includes both general mode
Synthesis of pyrrole-fused dibenzoxazepine/dibenzothiazepine/triazolobenzodiazepine derivatives via isocyanide-based multicomponent reactions
Beilstein J. Org. Chem. 2024, 20, 2870–2882, doi:10.3762/bjoc.20.241
- compounds with antibiotic, antiviral, and anticancer properties that are found in many drugs and natural products [1][2][3][4][5][6]. Pyrroles' biological properties manifest when they are fused to other heterocycles [7][8][9][10][11][12]. Among them, seven-membered heterocycles of the benzodiazepine
N-Glycosides of indigo, indirubin, and isoindigo: blue, red, and yellow sugars and their cancerostatic activity
Beilstein J. Org. Chem. 2024, 20, 2840–2869, doi:10.3762/bjoc.20.240
- anticancer activity of these compounds. Keywords: cancerostatic activity; carbohydrates; heterocycles; N-glycosides; indirubin; Introduction Indigo (1a), known for more than 6000 years and originally produced from indigo plants in India, represents a famous traditional blue pigment which was an expensive
- -rhamnosides α-17a and α-17c, respectively (Scheme 14) [23]. Water solubility plays an important role with regard to the pharmacological activity. It was previously shown that the water solubility and anticancer activity of non-glycosylated indirubins can be improved by conversion of the keto to an oxime group
- good activities were observed for both α-17a and β-17a. It is important to note that the anticancer activity of all indirubin-N-glycosides, in particular of rhamnosides α-17a and β-17a, was considerably higher as compared to the activities of previously reported non-glycosylated indirubins [23][24]. A
Synthesis of benzo[f]quinazoline-1,3(2H,4H)-diones
Beilstein J. Org. Chem. 2024, 20, 2708–2719, doi:10.3762/bjoc.20.228
- several drugs that are still important and often used. Examples include 5-fluorouracil and brivudine. 5-Fluoruracil is an important anticancer drug, while brivudine is considered to be one of the most effective antiviral drugs against the HSV-1 virus [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18
Transition-metal-free decarbonylation–oxidation of 3-arylbenzofuran-2(3H)-ones: access to 2-hydroxybenzophenones
Beilstein J. Org. Chem. 2024, 20, 2655–2667, doi:10.3762/bjoc.20.223
- anticancer effects [1]. Amongst these, 2-hydroxybenzophenones are regarded as one of the most important classes of compounds owing to their varied bioactivities, including calcium channel blockers, anti-influenza drugs, anti-HAV drugs, and antispasmodic agents (Figure 1) [2]. Along with that, oxybenzone, a 2
Synthesis, electrochemical properties, and antioxidant activity of sterically hindered catechols with 1,3,4-oxadiazole, 1,2,4-triazole, thiazole or pyridine fragments
Beilstein J. Org. Chem. 2024, 20, 2378–2391, doi:10.3762/bjoc.20.202
- (simeprevir, ritonavir, cobicistat), and other types of biological activities [15][16][17][18][19]. Besides, among the registered sulfur-containing drugs, 19% contain a thiazole ring, and 15% contain a thioether group [20]. Oxadiazole fragments are found in the structures of anticancer drugs (zibotentan
Tandem diazotization/cyclization approach for the synthesis of a fused 1,2,3-triazinone-furazan/furoxan heterocyclic system
Beilstein J. Org. Chem. 2024, 20, 2342–2348, doi:10.3762/bjoc.20.200
- , anticancer, non-steroidal anti-inflammatory, antihypertensive, antipsychotic, anxiolytic and in other pharmaceuticals [3][4][5]. Therefore, considering the diversity of biological properties, development of reliable approaches for the synthesis of new nitrogen heterocyclic systems is a highly urgent goal
- various diseases [17][18][19][20]. Therefore, due to their NO-releasing abilities, furoxan derivatives also demonstrate anticancer, antiplatelet, antiviral and antiparasitic properties [21][22][23][24][25][26][27][28][29][30][31][32]. Another valuable nitrogen heterocyclic scaffold in medicinal chemistry
Natural resorcylic lactones derived from alternariol
Beilstein J. Org. Chem. 2024, 20, 2171–2207, doi:10.3762/bjoc.20.187
- the detrimental effects of AOH [94][95][96]. AOH furthermore activated the nuclear translocation of the aryl hydrocarbon receptor (AhR) and the nuclear factor erythroid 2-related factor 2 (Nrf2) [97]. The possible anticancer effects of AOH through its cytotoxic, antiinflammatory, genotoxic, mutagenic
O,S,Se-containing Biginelli products based on cyclic β-ketosulfone and their postfunctionalization
Beilstein J. Org. Chem. 2024, 20, 2143–2151, doi:10.3762/bjoc.20.184
- regioselectivity to give diverse DHPMs in reasonable yields up to 95%. Moreover, an SO2-containing analogue of anticancer drug-candidate enastron (SO2 vs C=O) was obtained by using the here reported method in gram scale. We also demonstrate the reactivity of the Biginelli product in various directions – synthesis
- compounds with anticancer, antihypertensive, antiinflammatory, antioxidant, antimicrobial, antifungal, antimalarial, antitubercular, antidiabetic, antifilarial, anti-Alzheimer, antiepileptics and other activities [1][2][3][4][5][6][7][8][9][10][11]. The concept of "privileged structures" in medicinal
- -1,1-dioxide motif is presented in a number of biologically active compounds including important market drugs as antiglaucoma agent dorzolamide [21], diuretic/anticancer meticrane [22] and antiherpesvirus agent amenamevir (ASP-2151) [23] which was recently synthesized by Ugi-4CR [24] (Scheme 1C
Diastereoselective synthesis of highly substituted cyclohexanones and tetrahydrochromene-4-ones via conjugate addition of curcumins to arylidenemalonates
Beilstein J. Org. Chem. 2024, 20, 2016–2023, doi:10.3762/bjoc.20.177
- properties such as anticancer, anti-HIV protease, anti-ageing, anti-inflammatory and anti-oxidant, to name a few [12][13][14][15][16][17][18][19][20][21][22][23]. Considering the fact that curcumin’s uniqueness is associated with its ability to function as a multifunctional substrate in various organic
Allostreptopyrroles A–E, β-alkylpyrrole derivatives from an actinomycete Allostreptomyces sp. RD068384
Beilstein J. Org. Chem. 2024, 20, 1981–1987, doi:10.3762/bjoc.20.174
- by formyl and carboxyl functionalities. Compounds 1, 4, and 5 showed cytotoxicity against Kasumi-1 human acute myeloblastic leukemia cells with IC50 values of 103, 105, and 105 μM, respectively, which are less active than the anticancer agent cisplatin, with an IC50 value of 70 μM. Keywords
2-Heteroarylethylamines in medicinal chemistry: a review of 2-phenethylamine satellite chemical space
Beilstein J. Org. Chem. 2024, 20, 1880–1893, doi:10.3762/bjoc.20.163
- importance and applications of ring-modified histidines, Sharma et al. [66] reviewed the design, synthesis, and medicinal chemistry of these motifs covering antimicrobial, antiplasmodial, CNS and anticancer applications among others. Pyrazoles: Betazole (95) is a pyrazole-like histamine analogue with H2
The Groebke–Blackburn–Bienaymé reaction in its maturity: innovation and improvements since its 21st birthday (2019–2023)
Beilstein J. Org. Chem. 2024, 20, 1839–1879, doi:10.3762/bjoc.20.162
Discovery of antimicrobial peptides clostrisin and cellulosin from Clostridium: insights into their structures, co-localized biosynthetic gene clusters, and antibiotic activity
Beilstein J. Org. Chem. 2024, 20, 1800–1816, doi:10.3762/bjoc.20.159
- Acinetobacter baumannii [26], as supported by the current study. In addition, some lanthipeptides have been shown to have anticancer and immunomodulatory properties [11][27]. A low development of resistance to lanthipeptides has been observed, with nisin being the most well-known case in the food industry
Syntheses and medicinal chemistry of spiro heterocyclic steroids
Beilstein J. Org. Chem. 2024, 20, 1713–1745, doi:10.3762/bjoc.20.152
- Smoothened protein (Smo protein) [7]. The HH pathway, implicated in the development and progression of various human cancers (including colorectal, brain, gastrointestinal, lung, and breast cancers), drives tumorigenesis [8]. Consequently, HH pathway inhibitors have demonstrated significant anticancer
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