Synthesis and acaricidal activity against Varroa destructor of α- and γ-costic acid dimers

• Alessandro Santarsiere,
• Ernesto Santoro,
• Maria Letizia Ciavatta,
• Marianna Carbone,
• Sonia Ganassi,
• Cosimo Tedino,
• Antonio De Cristofaro,
• Antonio Evidente and
• Stefano Superchi

Beilstein J. Org. Chem. 2026, 22, 1088–1096, doi:10.3762/bjoc.22.87

• 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

• 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

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

• Ivan Lyutin,
• Grigory Kantin,
• Olga Bakulina and
• Dmitry Dar'in

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

The trans-influence in gold chemistry from a catalytic perspective

• Manfred Bochmann

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 anti-cancer activity of naphthalimide–organylselanyl conjugates

• Rajkumar Ravi and
• Selvakumar Karuthapandi

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

• methylseleninic acid (1) has emerged as a promising drug candidate for the treatment of triple-negative breast cancer (TNBC) [27]. In addition, the classical organoselenium compound diphenyl diselenide (2) has shown significant anticancer activity against the MDA-MB-231 breast cancer cell line [28]. Very recently

• , a 4-nitro-substituted benzylic diselenide 3 was reported to inhibit the Akt/mTOR and ERK pathways while suppressing NF-κB–mediated inflammation and invasiveness in TNBC cells [29]. On the other hand, naphthalimides (NAP) are well known for their potent anticancer activity, as exemplified by the

Design, synthesis and biological evaluation of 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines as selective cytotoxic agents against HeLa cells

• Maryna V. Kachaeva,
• Agnieszka B. Olejniczak,
• Marta Denel-Bobrowska,
• Victor V. Zhirnov,
• Yevheniia S. Velihina,
• Stepan G. Pilyo and
• Volodymyr S. Brovarets

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

• pairs) can increase water solubility and facilitate salt formation. Introducing amino groups into heterocycles can have a significant impact on the anticancer activity of a compound [4][5]. Many studies have investigated the anticancer potential of heterocycle derivatives containing cytisine, glucamine

Synthesis and characterization of a isothiouronium-calix[4]arene derivative: self-assembly and anticancer activity

• Giuseppe Granata,
• Loredana Ferreri,
• Claudia Giovanna Leotta,
• Giovanni Mario Pitari and
• Grazia Maria Letizia Consoli

Beilstein J. Org. Chem. 2025, 21, 2535–2541, doi:10.3762/bjoc.21.195

• and precise than current treatments. Numerous multivalent constructs have been reported in literature, both as compounds with intrinsic anticancer activity [4] and nanocarriers for anticancer drug delivery [5][6]. In the development of multivalent compounds, macrocyclic scaffolds such as cyclodextrins

• ][26]. A variety of calixarene-based nanoconstructs have been reported, including nanosystems with light-triggered anticancer activity [27], potential anticancer vaccine candidates [28], and nanocarriers for anticancer drug delivery [29][30][31][32][33]. Numerous bioactive groups have been introduced

• anticancer activity. The synthesis and structural characterization of compound 3 were carried out, and its self-assembly behavior in aqueous medium was investigated using dynamic light scattering (DLS) and electrophoretic light scattering (ELS). The anticancer potential of compound 3 was assessed in human

Discovery of cytotoxic indolo[1,2-c]quinazoline derivatives through scaffold-based design

• Daniil V. Khabarov,
• Valeria A. Litvinova,
• Lyubov G. Dezhenkova,
• Dmitry N. Kaluzhny,
• Alexander S. Tikhomirov and
• Andrey E. Shchekotikhin

Beilstein J. Org. Chem. 2025, 21, 2062–2071, doi:10.3762/bjoc.21.161

• (positions 5, 6, and 12) with anticancer activity, thereby establishing indolo[1,2-c]quinazolines as a novel and underexplored platform for drug discovery. Results and Discussion Planar polycyclic compounds including classical frameworks such as acridine, anthraquinone, naphthalenediimide, etc. demonstrate

Enantioselective desymmetrization strategy of prochiral 1,3-diols in natural product synthesis

• Lihua Wei,
• Rui Yang,
• Zhifeng Shi and
• Zhiqiang Ma

Beilstein J. Org. Chem. 2025, 21, 1932–1963, doi:10.3762/bjoc.21.151

• completed the total synthesis of salinosporamide A, a marine-derived natural product with anticancer activity, featuring an enzymatic desymmetrization (Scheme 17) [49]. To establish the C4 chiral center, prochiral diol 118 (prepared from known compound 117) was treated with lipase from Pseudomonas sp. (WAKO

Oxetanes: formation, reactivity and total syntheses of natural products

• Peter Gabko,
• Martin Kalník and
• Maroš Bella

Beilstein J. Org. Chem. 2025, 21, 1324–1373, doi:10.3762/bjoc.21.101

Recent advances in the electrochemical synthesis of organophosphorus compounds

• Babak Kaboudin,
• Milad Behroozi,
• Sepideh Sadighi and
• Fatemeh Asgharzadeh

Beilstein J. Org. Chem. 2025, 21, 770–797, doi:10.3762/bjoc.21.61

• products, which also exhibit enhanced anticancer activity. The reaction was carried out in an undivided cell where the anode was reticulated vitreous carbon (RVC), and the cathode was platinum. Mechanistic studies revealed that Cp2Fe plays the main role in the reaction, and the reaction did not proceed

Synthesis, structure, ionochromic and cytotoxic properties of new 2-(indolin-2-yl)-1,3-tropolones

• Yurii A. Sayapin,
• Eugeny A. Gusakov,
• Inna O. Tupaeva,
• Alexander D. Dubonosov,
• Igor V. Dorogan,
• Valery V. Tkachev,
• Anna S. Goncharova,
• Gennady V. Shilov,
• Natalia S. Kuznetsova,
• Svetlana Y. Filippova,
• Tatyana A. Krasnikova,
• Yanis A. Boumber,
• Alexey Y. Maksimov,
• Sergey M. Aldoshin and
• Vladimir I. Minkin

Beilstein J. Org. Chem. 2025, 21, 358–368, doi:10.3762/bjoc.21.26

• 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

Non-covalent organocatalyzed enantioselective cyclization reactions of α,β-unsaturated imines

• Sergio Torres-Oya and
• Mercedes Zurro

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

N-Glycosides of indigo, indirubin, and isoindigo: blue, red, and yellow sugars and their cancerostatic activity

• Peter Langer

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

The Groebke–Blackburn–Bienaymé reaction in its maturity: innovation and improvements since its 21st birthday (2019–2023)

• Cristina Martini,
• Muhammad Idham Darussalam Mardjan and
• Andrea Basso

Beilstein J. Org. Chem. 2024, 20, 1839–1879, doi:10.3762/bjoc.20.162

Syntheses and medicinal chemistry of spiro heterocyclic steroids

• Laura L. Romero-Hernández,
• Ana Isabel Ahuja-Casarín,
• Penélope Merino-Montiel,
• Sara Montiel-Smith,
• José Luis Vega-Báez and
• Jesús Sandoval-Ramírez

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

• activity. Synthesizing spiro heterocyclic steroids entails numerous methodologies. Although the inherent stereochemistry of steroids sometimes facilitates the production of a single diastereomer without the need for chiral auxiliaries, nevertheless, their synthesis remains challenging due to the creation

Chemo-enzymatic total synthesis: current approaches toward the integration of chemical and enzymatic transformations

• Ryo Tanifuji and
• Hiroki Oguri

Beilstein J. Org. Chem. 2024, 20, 1693–1712, doi:10.3762/bjoc.20.151

• hydroxy group of the aglycon. Cotylenin exhibits promising anticancer activity, and its diterpene aglycon, cotylenol (1), was isolated from the filamentous fungi such as Phomopsis amygdali and Cladosporium sp. 501-7W (Scheme 2A) [20][21][22]. Brassicicenes, differing in oxidation levels from 1, have been

Competing electrophilic substitution and oxidative polymerization of arylamines with selenium dioxide

• Vishnu Selladurai and
• Selvakumar Karuthapandi

Beilstein J. Org. Chem. 2024, 20, 1221–1235, doi:10.3762/bjoc.20.105

• as antioxidative [1][2], antimicrobial [3][4], and anticancer activity [5][6]. Several classes of organoselenium compounds are known to imitate the glutathione peroxidase [7][8][9][10][11]. Consequently, the development of new strategies for selenation of organic compounds has attracted considerable

A Diels–Alder probe for discovery of natural products containing furan moieties

• Alyssa S. Eggly,
• Namuunzul Otgontseren,
• Carson B. Roberts,
• Amir Y. Alwali,
• Haylie E. Hennigan and
• Elizabeth I. Parkinson

Beilstein J. Org. Chem. 2024, 20, 1001–1010, doi:10.3762/bjoc.20.88

• isolated from a sea sponge, Plakortis simplex [3][4]. Wortmannin, which also has a furan, was isolated from Penicillium wortmannin and shows anticancer activity via potent inhibition of phosphoinositide 3-kinase [5]. These are just a handful of the bioactive natural products containing furans that exist

Research progress on the pharmacological activity, biosynthetic pathways, and biosynthesis of crocins

• Zhongwei Hua,
• Nan Liu and
• Xiaohui Yan

Beilstein J. Org. Chem. 2024, 20, 741–752, doi:10.3762/bjoc.20.68

• -inflammatory properties, hepatorenal protection, and anticancer activity. They are often used as coloring and seasoning agents. Due to the limited content of crocins in plants and the high cost of chemical synthesis, the supply of crocins is insufficient to meet current demand. The biosynthetic pathways for

• alleviate gestational hypertension. Therefore, crocins have the potential to prevent pregnancy-induced hypertension [45]. Anticancer Crocins exhibit potent anticancer activity against various cancer cell lines. Jiang et al. found that crocins reduce the survival and activity of cervical cancer cells [46

• ]. Mollaei et al. observed an increased Bax/Bcl-2 ratio in crocin-treated cancer cells. Therefore, crocins are proposed to exert anticancer activity by promoting apoptosis of cancer cells [47]. This mechanism is consistent with the results of Hoshyar et al., who observed the apoptosis-promoting activity of

Combretastatins D series and analogues: from isolation, synthetic challenges and biological activities

• Jorge de Lima Neto and
• Paulo Henrique Menezes

Beilstein J. Org. Chem. 2023, 19, 399–427, doi:10.3762/bjoc.19.31

• these compounds in folk medicine for the treatment of different types of diseases, such as inflammatory processes, viral infections, metabolic disorders and some types of cancer [13][14][15][16][17][18][19]. The first biological studies of the combretastatin D series exploited their anticancer activity

An accelerated Rauhut–Currier dimerization enabled the synthesis of (±)-incarvilleatone and anticancer studies

• Tharun K. Kotammagari,
• Sweta Misra,
• Sayantan Paul,
• Sunita Kunte,
• Rajesh G. Gonnade,
• Manas K. Santra and
• Asish K. Bhattacharya

Beilstein J. Org. Chem. 2023, 19, 204–211, doi:10.3762/bjoc.19.19

• configuration of each enantiomer was determined by single-crystal X-ray analysis. In addition, a one-pot synthesis of (±)-incarviditone has been achieved from rac-rengyolone by using KHMDS as a base. We have also assessed the anticancer activity of all the synthesized compounds in breast cancer cells

• % yields, respectively, while Tang et al [4] furnished (±)-incarvilleatone (1) and (±)-incarviditone (2) from (±)-rengyolone (3) in 38% and 40% yields, respectively. A previous study [1] showed that (±)-incarviditone (2) has a limited anticancer activity. The anticancer activity is closely correlated with

Insight into oral amphiphilic cyclodextrin nanoparticles for colorectal cancer: comprehensive mathematical model of drug release kinetic studies and antitumoral efficacy in 3D spheroid colon tumors

• Sedat Ünal,
• Gamze Varan,
• Juan M. Benito,
• Yeşim Aktaş and
• Erem Bilensoy

Beilstein J. Org. Chem. 2023, 19, 139–157, doi:10.3762/bjoc.19.14

• -loaded nanoparticle formulations had better anticancer activity than the drug solution (Figure 5b). Moreover, the group treated with blank CS-(6-O-capro-β-CD) nanoparticles + CPT solution showed a substantial reduction in cell viability. Cell viability in HT29 cells cultured with CPT solution alone was

• the blank poly-β-CD-C6 nanoparticles plus CPT solution treated group had higher anticancer activity than the only drug solution treated group at the end of 72 hours. Furthermore, the anticancer activity of blank poly-β-CD-C6 nanoparticles was shown to be greater than that of the drug solution. It was

• cells respond differently to the treated groups [61][62][63]. Evaluation of antitumoral efficiency of CPT-loaded CD nanoparticles on 3D cell cultures Anticancer activity of nanoparticles prepared from different CD derivatives was also investigated in a 3D cell culture method. Matrigel® was used as the

Combining the best of both worlds: radical-based divergent total synthesis

• Kyriaki Gennaiou,
• Antonios Kelesidis,
• Maria Kourgiantaki and
• Alexandros L. Zografos

Beilstein J. Org. Chem. 2023, 19, 1–26, doi:10.3762/bjoc.19.1

• -fused tetracycle instead, were reported to possess NF-kB-inhibitory activity and anticancer activity against NCI H-929 cancer cell lines (Scheme 6) [39]. In 2021 Lu’s group reported the total synthesis of members of both meroterpenoid families based on a highly chemoselective α-alkylation in the

Selective sulfonylation and isonitrilation of para-quinone methides employing TosMIC as a source of sulfonyl group or isonitrile group

• Chuanhua Qu,
• Run Huang,
• Yong Li,
• Tong Liu,
• Yuan Chen and
• Guiting Song

Beilstein J. Org. Chem. 2021, 17, 2822–2831, doi:10.3762/bjoc.17.193

• , antimicrobial, antimalarial, and anticancer activities [1][2]. Diarylmethane motifs are widely present in natural products and pharmaceuticals that exhibit extraordinary biological activity [3][4] (Figure 1). Among them, their anticancer activity is particularly attractive, demonstrated by drugs such as

• letrozole [5] and entrectinib [6], with especially entrectinib showing a potent anticancer activity against a broad spectrum of human cancer cell lines. In recent decades, the construction of a hybrid system with varied biological and pharmaceutical activities has received extensive attention from medicinal

Highly stereocontrolled total synthesis of racemic codonopsinol B through isoxazolidine-4,5-diol vinylation

• Lukáš Ďurina,
• Anna Ďurinová,
• František Trejtnar,
• Ľuboš Janotka,
• Lucia Messingerová,
• Jana Doháňošová,
• Ján Moncol and
• Róbert Fischer

Beilstein J. Org. Chem. 2021, 17, 2781–2786, doi:10.3762/bjoc.17.188

• human cancer cell lines has never been described. In view of this, we have developed an efficient and highly diastereoselective approach towards codonopsinol B (1) and its N-nor-methyl analogue 2 from achiral starting materials and evaluated their anticancer activity using four different cancer cell