Building photoswitchable 3,4'-AMPB peptides: Probing chemical ligation methods with reducible azobenzene thioesters

• Gehad Zeyat and
• Karola Rück-Braun

Beilstein J. Org. Chem. 2012, 8, 890–896, doi:10.3762/bjoc.8.101

• cell surface receptor, belonging to the tumor-necrosis-factor receptor superfamily, which induces apoptosis. Fas-associated phosphatase-1 (FAP-1) is a Fas binding protein, which interacts with 12 to 15 of the C-terminal amino acids of the Fas receptor; however, the necessary and sufficient region for

• photoswitchable ligands. For instance, Fas-associated studies in certain cells using the tripeptide SLV suggest that this small peptide alone can induce apoptosis [14][15]. Related peptides containing class I C-terminal sequence motifs, e.g., SKV, are also derived from viral origins [16]. The latter specific

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

• Smo [14][15]. Cyclopamine can effectively induce a decrease in proliferation and an increase of apoptosis in several murine models [16][17]. However, the clinical development of cyclopamine as a therapeutic in cancer is hampered by its poor aqueous solubility (ca. 5 µg/mL) and acid lability

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

• ; 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

Toward an integrated route to the vernonia allenes and related sesquiterpenoids

• Da Xu,
• Michael A. Drahl and
• Lawrence J. Williams

Beilstein J. Org. Chem. 2011, 7, 937–943, doi:10.3762/bjoc.7.104

• terrestrial plants, algae, and insect pheromones that purportedly have anticancer, antifungal, and antibiotic activity, among others. For example, parthenolide (6) has anti-inflammatory and anti-hyperalgesic effects and induces apoptosis of human acute myelogenous leukemia stem and progenitor cells [24

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

• has also been approved for familial adenomatous polyposis demonstrating its ability to induce apoptosis in certain cancer cell lines [70]. As this activity is not shared with all COX-2 inhibitors, it is believed that the structural features such as the polar sulfonamide group, the lipophilic tolyl

• moiety and the trifluoromethylated pyrazole core with its negative electrostatic potential play a key role in apoptosis induction. Consequently, the anti-inflammatory and apoptosis inducing properties of celecoxib are assumed to result via different modes of action. In a recent study [71], celecoxib has

Synthesis and binding studies of two new macrocyclic receptors for the stereoselective recognition of dipeptides

• Ana Maria Castilla,
• M. Morgan Conn and
• Pablo Ballester

Beilstein J. Org. Chem. 2010, 6, No. 5, doi:10.3762/bjoc.6.5

• of protein–protein interactions is gaining interest as they are known to play a critical role in important biological processes such as the normal function of cellular/organelle structure, immune response, enzyme inhibitors, signal transduction, and apoptosis. Rational protein surface recognition

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

• ], antioxidant and anti-inflammatory agent [12][13][14] as well as induces apoptosis in human leukemia cell lines [15][16]. It is believed that broad spectrum of activities of Dan Shen are mainly associated with the presence of tetra cyclic furoquinone diterpenoids like Tanshinone I [17][18], Tanshinone IIA and

A short stereoselective synthesis of (+)-(6R,2′S)-cryptocaryalactone via ring- closing metathesis

• Palakodety Radha Krishna,
• Krishnarao Lopinti and
• K. L. N. Reddy

Beilstein J. Org. Chem. 2009, 5, No. 14, doi:10.3762/bjoc.5.14

• ], they inhibit HIV protease [8][9], induce apoptosis [10][11][12][13][14][15], and have even proved to be antileukemic [16]. At least some of these pharmacological effects may be related to the presence of the conjugated double bond, which acts as a Michael acceptor [17][18][19][20][21][22][23]. One of

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

• ]. Inhibition by these mechanisms results in adenosine triphosphate (ATP) deprivation, which leads to apoptosis of the highly energy demanding tumor cells [11]. The acetogenins are now considered as the most potent (effective in nanomolar concentrations) known inhibitors of the mitochondrial complex I [9][12

Stereoselective synthesis of (2S,3S,4Z)-4-fluoro- 1,3-dihydroxy- 2-(octadecanoylamino)octadec- 4-ene, [(Z)-4-fluoroceramide], and its phase behavior at the air/water interface

• Gergana S. Nikolova and
• Günter Haufe

Beilstein J. Org. Chem. 2008, 4, No. 12, doi:10.3762/bjoc.4.12

• in sphingolipid metabolism, sphingosine and its N-octadecanoyl-derivative, ceramide, exhibit a variety of biological functions. These compounds play a crucial role in many essential biological processes such as cell growth, cell differentiation, cell recognition and apoptosis. More specifically

• such as cell growth, cell differentiation, cell recognition and apoptosis [3][4][5][6][7][8][9]. Moreover, sphingosine is known as an inhibitor of protein kinase C [10][11]. The dynamic balance between ceramide, sphingosine and sphingosine-1-phosphate seems to be decisive for cell growth or apoptosis

• [12][13]. The specific initiation of apoptosis by suitable derivatives of these signal molecules is discussed as a new method for treatment of numerous diseases [1][14][15], and of cancer in particular [16][17][18]. A few years ago Herdewijn et al. showed that fluorinated ceramide and dihydroceramide

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

• when two microtubule-polymerizing agents were used, synergistic inhibition of microtubule dynamicity could be observed [46]. Paclitaxel and discodermolide also synergistically affected G2-M arrest, proliferation, and apoptosis [46]. Some workers speculate that such synergy might arise from the

• that cells enter apoptosis shortly after paclitaxel exposure, suggesting that they are directed into a cell death pathway before entering the mitotic phase of the cell cycle [52][53]. Conversely, certain cells treated at high concentrations could pass through mitosis but still avoid apoptosis. This was