Formal synthesis of (−)-agelastatin A: an iron(II)-mediated cyclization strategy

• Daisuke Shigeoka,
• Takuma Kamon and
• Takehiko Yoshimitsu

Beilstein J. Org. Chem. 2013, 9, 860–865, doi:10.3762/bjoc.9.99

• isolated from marine sponges Agelas dendromorpha and Cymbastela sp., is one such substance, which has drawn considerable attention due to its potential applicability in the development of anticancer agents [1][2][3][4][5]. The intriguing biological activity of 1 has stimulated interest in developing

The diketopiperazine-fused tetrahydro-β-carboline scaffold as a model peptidomimetic with an unusual α-turn secondary structure

• Francesco Airaghi,
• Andrea Fiorati,
• Giordano Lesma,
• Manuele Musolino,
• Alessandro Sacchetti and
• Alessandra Silvani

Beilstein J. Org. Chem. 2013, 9, 147–154, doi:10.3762/bjoc.9.17

• attention in recent years because of their broad biological activities [11][12] and therapeutic applications, ranging from antibiotics [13] to anticancer agents [14]. Moreover, the DKP moiety has been exploited as a peptidomimetic scaffold [15][16][17]. Structural unification of THBC and DKP pharmacophores

A new synthetic access to 2-N-(glycosyl)thiosemicarbazides from 3-N-(glycosyl)oxadiazolinethiones and the regioselectivity of the glycosylation of their oxadiazolinethione precursors

• El Sayed H. El Ashry,
• El Sayed H. El Tamany,
• Mohy El Din Abdel Fattah,
• Mohamed R. E. Aly,
• Ahmed T. A. Boraei and
• Axel Duerkop

Beilstein J. Org. Chem. 2013, 9, 135–146, doi:10.3762/bjoc.9.16

• acid. This is known as a metabolic cell-surface-engineering technique for cell-surface interactions and consequently shows the potential of these compounds for the development of anticancer agents [13][14][15][16]. Antituberculosis effects of glycosylthiosemicarbazides were also reviewed [17

Bioactive selaginellins from Selaginella tamariscina (Beauv.) Spring

• Chao Yang,
• Yutian Shao,
• Kang Li and
• Wujiong Xia

Beilstein J. Org. Chem. 2012, 8, 1884–1889, doi:10.3762/bjoc.8.217

• were assigned in Table 2. Several species of the genus Selaginella have long been used in traditional medicine as anticancer agents, but only limited literature information on the cytotoxic activity of their constituents is available, which encourages us to investigate the cytotoxic effect of the

• more potent and selective selaginellin analogues and their biogenetic precursors. Additional controlled studies are needed to investigate the efficacy and safety of selaginellins as antioxidant and anticancer agents. Experimental General experimental procedures. IR spectra were measured on a Perkin

An intramolecular inverse electron demand Diels–Alder approach to annulated α-carbolines

• Zhiyuan Ma,
• Feng Ni,
• Grace H. C. Woo,
• Sie-Mun Lo,
• Philip M. Roveto,
• Scott E. Schaus and
• John K. Snyder

Beilstein J. Org. Chem. 2012, 8, 829–840, doi:10.3762/bjoc.8.93

• ], inhibitors of ApoB-100-associated lipoprotein production for cholesterol lowering [21], and more recently, as inhibitors of CDK1 kinase as potential anticancer agents [22]. This later filing has triggered investigations into α-carbolines as potential multikinase inhibitors [23]. Existing synthetic approaches

Syntheses and applications of furanyl-functionalised 2,2’:6’,2’’-terpyridines

• Jérôme Husson and
• Michael Knorr

Beilstein J. Org. Chem. 2012, 8, 379–389, doi:10.3762/bjoc.8.41

• -substituted terpyridines in biomedical sciences Furanyl-terpyridines were probed in biomedical sciences as cytotoxic molecules. Compounds 12 and 13 were tested as anticancer agents against seven different cell lines [4]. Their activities were compared to that of doxorubicin, which is a currently used

Efficient syntheses of 25,26-dihydrodictyostatin and 25,26-dihydro-6-epi-dictyostatin, two potent new microtubule-stabilizing agents

• María Jiménez,
• Wei Zhu,
• Andreas Vogt,
• Billy W. Day and
• Dennis P. Curran

Beilstein J. Org. Chem. 2011, 7, 1372–1378, doi:10.3762/bjoc.7.161

• –Wadsworth–Emmons reaction sequence and an esterification. A late stage Nozaki–Hiyama–Kishi reaction was then used to form the 22-membered macrolide. The stereoselectivity of this reaction depended on the configurations of the nearby stereocenter at C6. Keywords: anticancer agents; dictyostatin

• ; microtubules; NHK; Introduction The discovery of compounds that function as anticancer agents by altering the dynamics of microtubules continues to be an important goal in medicinal chemistry. Such agents can force the cell to exit mitosis aberrantly, leading to apoptosis [1][2]. Important classes of

• ) (Figure 1). The later parts of this synthesis have been briefly communicated in a recent paper whose primary focus was biological evaluation [30]. Indeed, 3a and 3b prove to be promising anticancer agents with in vitro and cellular testing data superior to those of the 16-desmethyl analogs 2a and 2b, and

Synthesis of diverse dihydropyrimidine-related scaffolds by fluorous benzaldehyde-based Biginelli reaction and post-condensation modifications

• Bruno Piqani and
• Wei Zhang

Beilstein J. Org. Chem. 2011, 7, 1294–1298, doi:10.3762/bjoc.7.150

• ; Introduction Dihydropyrimidinone and dihydropyrimidine derivatives have broad biologically activities. Many synthetic samples have been studied as antibacterial, antiviral, antihypertensive, and anticancer agents [1], and the natural products containing these heterocyclic moieties have been studied as new

Synthesis, reactivity and biological activity of 5-alkoxymethyluracil analogues

• Lucie Brulikova and
• Jan Hlavac

Beilstein J. Org. Chem. 2011, 7, 678–698, doi:10.3762/bjoc.7.80

• applications in anticancer treatments and antiviral chemotherapy. In anticancer chemotherapy the huge amount of knowledge concerning processes taking place through the cell cycle has enabled researchers to break through and to understand the mechanisms of action of many anticancer agents. 5-Fluorouracil, for

• by fluorine have been investigated as potent anticancer agents since the 1960s. Nevertheless, many such modified compounds were also synthesized in order to investigate their antiviral activity. As a consequence of interest in biologically active fluoro derivatives, Bergstrom and co-workers carried

C–C (alkynylation) vs C–O (ether) bond formation under Pd/C–Cu catalysis: synthesis and pharmacological evaluation of 4-alkynylthieno[2,3-d]pyrimidines

• Dhilli Rao Gorja,
• K. Shiva Kumar,
• K. Mukkanti and
• Manojit Pal

Beilstein J. Org. Chem. 2011, 7, 338–345, doi:10.3762/bjoc.7.44

• that 4-alkynylthieno[2,3-d]pyrimidine can be used as a template for the identification of novel and potential anticancer agents. Conclusion In conclusion, the present study demonstrates the first efficient synthesis 4-alkynylthieno[2,3-d]pyrimidines in good to excellent yields. The combination of Pd/C

Approaches towards the synthesis of 5-aminopyrazoles

• Ranjana Aggarwal,
• Vinod Kumar,
• Rajiv Kumar and
• Shiv P. Singh

Beilstein J. Org. Chem. 2011, 7, 179–197, doi:10.3762/bjoc.7.25

• spectrum [12]. Recently, components of the mitotic machinery have been targeted in an attempt to develop novel anticancer agents. These include critical signaling kinases such as the Aurora, PLK, and the cyclin-dependent kinases (CDK). Compound VII (AZD1152) is the first Aurora-B selective inhibitor to