Amyloid-β probes: Review of structure–activity and brain-kinetics relationships

• Todd J. Eckroat,
• Abdelrahman S. Mayhoub and
• Sylvie Garneau-Tsodikova

Beilstein J. Org. Chem. 2013, 9, 1012–1044, doi:10.3762/bjoc.9.116

• . Between 2000 and 2008, the number of deaths caused by AD increased by 66%, a dramatic rise, especially when compared to other causes of death, such as heart disease, stroke, prostate and breast cancer, and HIV, which decreased by 3–29% during that time period [1]. As these numbers indicate, AD represents

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

• still retained affinity for tumor Hsp90, they were each evaluated in a fluorescence polarization (FP) assay by using a cancer-cell homogenate (i.e., SKBr3 human breast cancer lysate). This assay measures competitive binding to tumor cell Hsp90 complexes [23]. Each compound retained a good affinity for

• , Breast Cancer Research Fund, W.H. Goodwin and A. Goodwin and the Commonwealth Cancer Foundation for Research, The Experimental Therapeutics Center of Memorial Sloan-Kettering Cancer Center (MSKCC), 1U01 AG032969-01A1, 1R21 CA158609-01A1, 1R21 AI090501 and 1R01 CA155226-01. T.T. is funded by Susan G

• . Komen for the Cure (KG091313) and the Department of Defense, Breast Cancer Research Program (PDF-BC093421). We also thank Dr. George Sukenick and Dr. Hui Liu of the NMR Analytical Core Facility at MSKCC for expert mass spectral analysis.

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

• Matthias G. J. Baud,
• Thomas Leiser,
• Vanessa Petrucci,
• Mekala Gunaratnam,
• Stephen Neidle,
• Franz-Josef Meyer-Almes and
• Matthew J. Fuchter

Beilstein J. Org. Chem. 2013, 9, 81–88, doi:10.3762/bjoc.9.11

• potency ranking for the AB system: NOH > NOMe > O. The most sensitive cell line to treatment was the MCF7 breast cancer cell line, with the most potent thioester 8 displaying an IC50 of 3.2 μM. Such sensitivity correlates with previous SAR data [20]. While being moderately potent against MCF7 cells (21 μM

Cyclodextrin-based nanosponges as drug carriers

• Francesco Trotta,
• Marco Zanetti and
• Roberta Cavalli

Beilstein J. Org. Chem. 2012, 8, 2091–2099, doi:10.3762/bjoc.8.235

• available on the market. Nanosponge formulation could thus increase the bioavailability of itraconazole. The solubilisation efficiency of nanosponges with regard to tamoxifen, a nonsteroidal anti-estrogen molecule used for treating and preventing breast cancer, was observed by using a 0.5% aqueous

Modulating the activity of short arginine-tryptophan containing antibacterial peptides with N-terminal metallocenoyl groups

• H. Bauke Albada,
• Alina-Iulia Chiriac,
• Michaela Wenzel,
• Maya Penkova,
• Julia E. Bandow,
• Hans-Georg Sahl and
• Nils Metzler-Nolte

Beilstein J. Org. Chem. 2012, 8, 1753–1764, doi:10.3762/bjoc.8.200

• )3 and RcCO-W(RW)2 synAMPs against human red blood cells (hRBCs). IC50 values (in µM) of both (RW)3 and RcCO-W(RW)2 against human liver carcinoma (HepG2), human colon cancer (HT29) and human breast cancer (MCF7) cell lines. Acknowledgements We thank Annegret Knüfer for determining the IC50 values of

Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors

• Chao Che,
• Song Li,
• Bo Yang,
• Shengchang Xin,
• Zhixiong Yu,
• Taofeng Shao,
• Chuanye Tao,
• Shuo Lin and
• Zhen Yang

Beilstein J. Org. Chem. 2012, 8, 841–849, doi:10.3762/bjoc.8.94

• cancer, breast cancer and multiple myeloma [4][5][6][7][8][9]. Taken together, the development of Hh pathway antagonists has thus represented an attractive strategy for anticancer therapy [10][11]. Because mutated Ptch or Smo proteins are mostly responsible for the abnormal activation of Hh related to

Synthetic glycopeptides and glycoproteins with applications in biological research

• Ulrika Westerlind

Beilstein J. Org. Chem. 2012, 8, 804–818, doi:10.3762/bjoc.8.90

• present in the vaccines. FACS analysis with serum antibodies induced by the MUC1 vaccines 7–10 showed that they all recognize MCF-7 breast-cancer cells. The serum from mice immunized with vaccine 9 was further evaluated through mammary carcinoma tissue-staining experiments. A gradual increase of the

• of a MUC1 TN-glycopeptide, a polio peptide T-cell epitope and the Pam3CSK4 lipopeptide immune-stimulant was prepared by liposome-mediated native chemical ligation. Mice immunized with the three-component vaccine were injected with breast-cancer tumor cells, and were found to be significantly more

Identification and isolation of insecticidal oxazoles from Pseudomonas spp.

• Florian Grundmann,
• Veronika Dill,
• Andrea Dowling,
• Aunchalee Thanwisai,
• Edna Bode,
• Narisara Chantratita,
• Richard ffrench-Constant and
• Helge B. Bode

Beilstein J. Org. Chem. 2012, 8, 749–752, doi:10.3762/bjoc.8.85

• tested the bioactivity against the human breast-cancer cell line MCF-7, using the XTT assay [18], and against insect hemocytes from the greater wax moth Galleria melonella according to the method described by Proschak et al. [19]. Three oxazole compounds show LD50 [µg ml−1] values against Galleria

Synthesis and characterization of new diiodocoumarin derivatives with promising antimicrobial activities

• Hany M. Mohamed,
• Ashraf H. F. Abd EL-Wahab,
• Ahmed M. EL-Agrody,
• Ahmed H. Bedair,
• Fathy A. Eid,
• Mostafa M. Khafagy and
• Kamal A. Abd-EL-Rehem

Beilstein J. Org. Chem. 2011, 7, 1688–1696, doi:10.3762/bjoc.7.199

• their antidepressant, antithrombotic, antipsychotic (for the central nervous system, CNS) and anti-breast-cancer activities [13]. In view of the important biological properties of the diiodocoumarin derivatives and iodo-organic compounds as medical agents, we planned to synthesize some new

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

• -up and in vivo testing [28]. Indeed, 1b proved to be more effective than paclitaxel in treating mice bearing human breast cancer xenografts. Encouraged by these results, we have pursued both new analogs and improved synthetic routes. We recently reported a streamlined synthesis of dictyostatin (1a

• comparable to (−)-dictyostatin and discodermolide. Each compound also inhibited the growth of cell lines resistant to paclitaxel and epothilone B at low nanomolar concentrations, synergized with paclitaxel in MDA-MB-231 human breast cancer cells, and had anti-angiogenic activity in transgenic zebra fish

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

• the heterocycle. In general, the triazole containing drugs belong to two groups of therapeutic agents: selective and non-steroidal aromatase inhibitors which are used in the treatment of early and advanced breast cancer in postmenopausal women, e.g., letrozole (256, Femara) and anastrozole (257

Michael-type addition of azoles of broad-scale acidity to methyl acrylate

• Sławomir Boncel,
• Kinga Saletra,
• Barbara Hefczyc and
• Krzysztof Z. Walczak

Beilstein J. Org. Chem. 2011, 7, 173–178, doi:10.3762/bjoc.7.24

• -3,5-diyl)diphenol (IV) and its derivatives are known modulators of receptors regulating the secretion of estrogens crucial in the pathogenesis of breast cancer [4]. 4-(Benzo[d][1,3]dioxol-5-ylmethyl)-1-(3-methoxybenzyl)-3-phenyl-pyrazole-5-carboxylic acid (V) is an antagonist of endothelial receptors

Total synthesis of (±)-coerulescine and (±)-horsfiline

• Mukund G. Kulkarni,
• Attrimuni P. Dhondge,
• Sanjay W. Chavhan,
• Ajit S. Borhade,
• Yunnus B. Shaikh,
• Deekshaputra R. Birhade,
• Mayur P. Desai and
• Nagorao R. Dhatrak

Beilstein J. Org. Chem. 2010, 6, 876–879, doi:10.3762/bjoc.6.103

• against human breast cancer cells. This work led to intense interest in the total synthesis of these alkaloids and their derivatives. Despite previous intensive studies, the total synthesis of coerulescine (1) and horsfiline (2) remain attractive targets for demonstrating the efficacy of newer synthetic

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

Recent progress on the total synthesis of acetogenins from Annonaceae

• Nianguang Li,
• Zhihao Shi,
• Yuping Tang,
• Jianwei Chen and
• Xiang Li

Beilstein J. Org. Chem. 2008, 4, No. 48, doi:10.3762/bjoc.4.48

• 232, which has served as an intermediate in a total synthesis of uvaricin (225). Total synthesis of trilobin Trilobin (233), which was isolated from the the bark of Asimina triloba by McLaughlin’s group [71] in 1992, has high potency against human lung cancer, breast cancer, and colon cancer cell

Transition- metal/Lewis acid free synthesis of acyl benzothiophenes via C-C bond forming reaction

• Sarbani Pal,
• Mohammad Ashrafuddin Khan,
• P. Bindu and
• P. K. Dubey

Beilstein J. Org. Chem. 2007, 3, No. 35, doi:10.1186/1860-5397-3-35

• lipids while displaying potent estrogen antagonist properties in the breast and uterus. A most common example of SERM is tamoxifen which has been the therapy of choice in the endocrine treatment of all stages of hormone-dependent breast cancer and in the primary and secondary chemoprevention of breast

• cancer. Recently, raloxifene showed promising results in clinical trial and is expected to provide an alternative to current hormone replacement therapy (HRT) that has been causally linked to breast cancer.[2] Another compound B (Figure 1) was identified as a thrombin inhibitor that could be utilized in

Cimicifoetisides A and B, two cytotoxic cycloartane triterpenoid glycosides from the rhizomes of Cimicifuga foetida, inhibit proliferation of cancer cells

• Li-Rong Sun,
• Chen Qing,
• Yan-Li Zhang,
• Shu-Yu Jia,
• Zhong-Rong Li,
• Shen-Ji Pei,
• Ming-Hua Qiu,
• Michael L. Gross and
• Samuel X. Qiu

Beilstein J. Org. Chem. 2007, 3, No. 3, doi:10.1186/1860-5397-3-3

• cytotoxicity against rat EAC (Ehrlich ascites carcinoma) and MDA-MB-A231 (human breast cancer) cells with IC50 values of 0.52 and 6.74 μM for 1, and 0.19 and 10.21 μM for 2, suggesting their potential for further investigation as anti-cancer agents. 1. Background Black cohosh (Cimicifuga racemosa (L.) Nutt

• significant cytotoxicity against the rat EAC tumor cell line with IC50 values of 0.35 and 0.14 μg/ml for 1 and 2, respectively. Both 1 and 2 also demonstrated moderate inhibition to human MDA-MB-A231 breast cancer cell. While other compounds were shown to be devoid of significant cytotoxicity, implying the

• the potential for further examination of the cycloartane triterpene glycosides from Cimicifuga for the prevention or treatment of human cancers, especially for breast cancer. It should be noted that the extracts of Cimicifuga are currently widely available for sale as a dietary supplements used for