C-5’-Triazolyl-2’-oxa-3’-aza-4’a-carbanucleosides: Synthesis and biological evaluation

• Roberto Romeo,
• Caterina Carnovale,
• Salvatore V. Giofrè,
• Maria A. Chiacchio,
• Adriana Garozzo,
• Emanuele Amata,
• Giovanni Romeo and
• Ugo Chiacchio

Beilstein J. Org. Chem. 2015, 11, 328–334, doi:10.3762/bjoc.11.38

• ]: Some of these compounds show a good anticancer activity against the anaplastic (8305C) and the follicular (FTC-133) human thyroid cancer cell lines, and especially on the U87MG human primary glioblastoma cell line (Figure 2). Accordingly, considering that the incorporation of the triazole moiety can

Natural phenolic metabolites with anti-angiogenic properties – a review from the chemical point of view

• Qiu Sun,
• Jörg Heilmann and
• Burkhard König

Beilstein J. Org. Chem. 2015, 11, 249–264, doi:10.3762/bjoc.11.28

• -glucuronidase activity is possible [86]. Fisetin can be found in many fruits such as strawberries and apples (Malus spec. MILL., Rosaceae) as well as in vegetables such as onions (Allium cepa L., Amaryllidaceae, subfamily Allioideae former family Alliaceae). It shows anticancer activity in various cancer models

Formation of nanoparticles by cooperative inclusion between (S)-camptothecin-modified dextrans and β-cyclodextrin polymers

• Thorbjørn Terndrup Nielsen,
• Catherine Amiel,
• Laurent Duroux,
• Kim Lambertsen Larsen,
• Lars Wagner Städe,
• Reinhard Wimmer and
• Véronique Wintgens

Beilstein J. Org. Chem. 2015, 11, 147–154, doi:10.3762/bjoc.11.14

• potent anticancer activity by inhibition of topoisomerase II. Its major drawback is its extremely low aqueous solubility of 2.5 µg/mL leading to a low bioavailability and it is thus a considerable formulation challenge [4]. Furthermore, at physiological conditions its active lactone form is hydrolysed to

Inclusion of trans-resveratrol in methylated cyclodextrins: synthesis and solid-state structures

• Lee Trollope,
• Dyanne L. Cruickshank,
• Terence Noonan,
• Susan A. Bourne,
• Milena Sorrenti,
• Laura Catenacci and
• Mino R. Caira

Beilstein J. Org. Chem. 2014, 10, 3136–3151, doi:10.3762/bjoc.10.331

• benefits exhibited by RSV (including, e.g., anti-inflammatory effects, cardiovascular protection, and anticancer activity [3]) has increased considerably. Its low aqueous solubility, however, is one of the factors that limits its utility [4] and various methods have been employed to address this

Chemistry of polyhalogenated nitrobutadienes, 14: Efficient synthesis of functionalized (Z)-2-allylidenethiazolidin-4-ones

• Viktor A. Zapol’skii,
• Jan C. Namyslo,
• Mimoza Gjikaj and
• Dieter E. Kaufmann

Beilstein J. Org. Chem. 2014, 10, 1638–1644, doi:10.3762/bjoc.10.170

• -inhibiting and antialgal properties [49], show anticancer activity [50][51], and are inhibitors of bacterial enzyme synthetase MurD with E. coli [52]. Additional treatment of thiazolidin-4-one 8 with a fivefold excess of hydrazine hydrate resulted in the formation of a 1H-pyrazole: A total of two hydrazine

C–H-Functionalization logic guides the synthesis of a carbacyclopamine analog

• Sebastian Rabe,
• Johann Moschner,
• Marina Bantzi,
• Philipp Heretsch and
• Athanassios Giannis

Beilstein J. Org. Chem. 2014, 10, 1564–1569, doi:10.3762/bjoc.10.161

• interest from research groups in biology, chemistry and medicine [1][2][3][4]. As the first identified hedgehog signaling inhibitor, cyclopamine exerts its anticancer activity through a novel mechanism of action, which manifests itself in its remarkable activity against several types of human cancer

Synthesis of indole-based propellane derivatives via Weiss–Cook condensation, Fischer indole cyclization, and ring-closing metathesis as key steps

• Sambasivarao Kotha,
• Ajay Kumar Chinnam and
• Arti Tiwari

Beilstein J. Org. Chem. 2013, 9, 2709–2714, doi:10.3762/bjoc.9.307

• vincristine-resistant KB cancer cells [23][24]. Minfiensine alkaloid [25][26][27][28][29][30][31] containing a novel 1,2,3,4-tetrahydrocarbazole ring skeleton shows anticancer activity [32]. König and co-workers identified some propellane derivatives as cannabinoid CB1 receptor antagonists [33], which are

Mild and efficient cyanuric chloride catalyzed Pictet–Spengler reaction

• Ashish Sharma,
• Mrityunjay Singh,
• Nitya Nand Rai and
• Devesh Sawant

Beilstein J. Org. Chem. 2013, 9, 1235–1242, doi:10.3762/bjoc.9.140

• with aldehydes furnished tetrahydro-β-carboline 3 and indolo[1,2-a]quinoxaline 8, respectively. The β-carboline skeleton is widely distributed in marine organisms [54][55][56]. Eudistomine and manzamine isolated from marine invertebrates exhibited promising anticancer activity [57][58]. Tedalafil, a

Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes

• Tony Taldone,
• Anna Rodina,
• Erica M. DaGama Gomes,
• Matthew Riolo,
• Hardik J. Patel,
• Raul Alonso-Sabadell,
• Danuta Zatorska,
• Maulik R. Patel,
• Sarah Kishinevsky and
• Gabriela Chiosis

Beilstein J. Org. Chem. 2013, 9, 544–556, doi:10.3762/bjoc.9.60

• molecule to investigate Hsp90 biology, and in fact the attachment of GM to solid support enabled the identification of Hsp90 as the target of its anticancer activity through affinity purification [16]. Biotinylated GM has also been synthesized and has been proposed as a tool to identify proteins other than

Hydrophobic analogues of rhodamine B and rhodamine 101: potent fluorescent probes of mitochondria in living C. elegans

• Laurie F. Mottram,
• Safiyyah Forbes,
• Brian D. Ackley and
• Blake R. Peterson

Beilstein J. Org. Chem. 2012, 8, 2156–2165, doi:10.3762/bjoc.8.243

• rosamines can confer selective anticancer activity both in vitro and in vivo in animal models [13]. Under nontoxic conditions, rhodamines and mitochondria-targeted fluorescent proteins have been extensively used for imaging and analysis of these organelles in cell culture, enabling studies of dynamic fusion

Enantioselective supramolecular devices in the gas phase. Resorcin[4]arene as a model system

• Caterina Fraschetti,
• Matthias C. Letzel,
• Antonello Filippi,
• Maurizio Speranza and
• Jochen Mattay

Beilstein J. Org. Chem. 2012, 8, 539–550, doi:10.3762/bjoc.8.62

• the anticancer activity, by focusing on the drug/receptor interaction. Vinblastine and vincristine are “dimeric” molecules, comprising two subunits, i.e., rearranged (+)-catharanthine (T) and (−)-vindoline (D) (Figure 4) [48]. The gas-phase ligand-displacement approach was employed to investigate the

Functional properties of metallomesogens modulated by molecular and supramolecular exotic arrangements

• Alessandra Crispini,
• Mauro Ghedini and
• Daniela Pucci

Beilstein J. Org. Chem. 2009, 5, No. 54, doi:10.3762/bjoc.5.54

• while the half-disc-shaped curcuminoids (B in Figure 2) self-assemble with the formation of columnar mesophases. Moreover, the presence of biologicaly active fragments (the O,O chelating ligands) induces promising anticancer activity in vitro against two human prostatic cancer cell lines in all these

Studies on polynuclear furoquinones. Part 1: Synthesis of tri- and tetra- cyclic furoquinones simulating BCD/ABCD ring system of furoquinone diterpenoids

• Faruk H. Shaik and
• Gandhi K. Kar

Beilstein J. Org. Chem. 2009, 5, No. 47, doi:10.3762/bjoc.5.47

• viral hepatitis, cardiac and vascular disorder, hypertension, miscarriage and menstrual disorder [3][9] etc. It has been reported to show potential anticancer activity [10] (against human breast cancer), cytotoxic and antiplatelet aggregation activities [1][11]. It also acts as an antibacterial [1

Colchitaxel, a coupled compound made from microtubule inhibitors colchicine and paclitaxel

• Karunananda Bombuwala,
• Thomas Kinstle,
• Vladimir Popik,
• Sonal O. Uppal,
• James B. Olesen,
• Jose Viña and
• Carol A. Heckman

Beilstein J. Org. Chem. 2006, 2, No. 13, doi:10.1186/1860-5397-2-13

• that they have potent anticancer activity. Although the inhibitor combinations are thought to be effective because they interfere with chromosome separation by two separate microtubule-related mechanisms, there is also evidence that another mechanism of synergy may exist (see Discussion). In an assay