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The German National Case Collection for Familial Pancreatic Carcinoma (FaPaCa)—Knowledge Gained in 20 Years.

Detlef Klaus Bartsch, Elvira Matthäi, Ioannis Mintziras, Christian Bauer, Jens Figiel, Mercede Sina-Boemers, Thomas M Gress, Peter Langer, Emily P Slater,

<h4>Background</h4>Familial pancreatic carcinoma (FPC) is a rare hereditary tumor syndrome with a heterogeneous clinical phenotype. The study of FPC also contributes to a better understanding of the more common sporadic pancreatic ductal adenocarcinoma (PDAC). We report on the past 20 years' experience of the German National Case Collection for Familial ... Read more >>

Dtsch Arztebl Int (Deutsches Arzteblatt international)
[2021, 118(Forthcoming):]

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Synthesis of 2-Azapyrenes and Their Photophysical and Electrochemical Properties.

Ricardo Molenda, Sebastian Boldt, Alexander Villinger, Peter Ehlers, Peter Langer,

A series of 5,7,9-substituted 2-azapyrenes were synthesized for the first time. The synthesis relies on Brønsted acid promoted benzannulation of alkyne precursors prepared by palladium-catalyzed cross-coupling reactions. The synthetic strategy is efficient and the scope covers a variety of functional groups. The electrochemical behavior and photophysical properties of the products ... Read more >>

J Org Chem (The Journal of organic chemistry)
[2020, 85(20):12823-12842]

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Synthesis of thieno[2,3-h]-/[3,2-h]quinolines and thieno[2,3-f] quinolines by Brønsted acid mediated cycloisomerisation.

Marian Blanco Ponce, Eugenio Torres Rodríguez, Anika Flader, Peter Ehlers, Peter Langer,

Several thieno[2,3-h]-/[3,2-h]- and [2,3-f]quinolines have been synthesised from 2,3-dihalogenated pyridines or -quinolines by site-selective Pd catalysed cross-coupling reactions and Brønsted acid mediated cycloisomerisations as the final key step. This newly developed synthetic strategy is used in a modular way to synthesize diverse regioisomeric derivatives, tolerates various functional groups, and proceeds ... Read more >>

Org Biomol Chem (Organic & biomolecular chemistry)
[2020, 18(33):6531-6536]

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Structure-based virtual screening of dipeptidyl peptidase 4 inhibitors and their in vitro analysis.

Shafiq Ur Rahman, Hafiz Saqib Ali, Behzad Jafari, Sumera Zaib, Abdul Hameed, Yasser M S A Al-Kahraman, Peter Langer, Jamshed Iqbal,

Type 2 diabetes mellitus (T2DM) is one of the most widely prevalent metabolic disorders with no cure to date thus remains the most challenging task in the current drug discovery. Therefore, the only strategy to control diabetes prevalence is to develop novel efficacious therapeutics. Dipeptidyl Peptidase 4 (DPP-4) inhibitors are ... Read more >>

Comput Biol Chem (Computational biology and chemistry)
[2020, :107326]

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The rise of one anastomosis gastric bypass: insights from surgeons and dietitians.

Osnat Kaniel, Amir Szold, Nasser Sakran, Nasser Sakran, Yafit Kessler, Peter Langer, Tair Ben-Porat, Jacob Moran-Gilad, Shiri Sherf-Dagan,

One anastomosis gastric bypass/Mini Gastric Bypass (OAGB/MGB) is an emerging bariatric surgery (BS) technique. We evaluated and compared attitudes of bariatric surgeons and dietitians towards the considerations for choosing BS-type ("Decision-making"), the contributing factors to the rise of OAGB/MGB in Israel ("OAGB/MGB-rise") and notions regarding the occurrence of gastrointestinal (GI) ... Read more >>

Updates Surg (Updates in surgery)
[2020, :]

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Palladium-catalyzed synthesis and nucleotide pyrophosphatase inhibition of benzo[4,5]furo[3,2-b]indoles.

Hoang Huy Do, Saif Ullah, Alexander Villinger, Joanna Lecka, Jean Sévigny, Peter Ehlers, Jamshed Iqbal, Peter Langer,

A two-step palladium-catalyzed procedure based on Suzuki-Miyaura cross coupling, followed by a double Buchwald-Hartwig reaction, allows for the synthesis of pharmaceutically relevant benzo[4,5]furo[3,2-b]indoles in moderate to very good yield. The synthesized compounds have been analyzed with regard to their inhibitory activity (IC50) of nucleotide pyrophosphatases h-NPP1 and h-NPP3. The activity ... Read more >>

Beilstein J Org Chem (Beilstein journal of organic chemistry)
[2019, 15:2830-2839]

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Highly Potent and Selective Ectonucleoside Triphosphate Diphosphohydrolase (ENTPDase1, 2, 3 and 8) Inhibitors Having 2-substituted-7- trifluoromethyl-thiadiazolopyrimidones Scaffold.

Saira Afzal, Sumera Zaib, Behzad Jafari, Peter Langer, Joanna Lecka, Jean Sévigny, Jamshed Iqbal,

<h4>Background</h4>The ecto-nucleoside triphosphate diphosphohydrolases (NTPDases) terminate nucleotide signaling via the hydrolysis of extracellular nucleoside-5'-triphosphate and nucleoside- 5'-diphosphate, to nucleoside-5'-monophosphate and composed of eight Ca2+/Mg2+ dependent ectonucleotidases (NTPDase1-8). Extracellular nucleotides are involved in a variety of physiological mechanisms. However, they are rapidly inactivated by ectonucleotidases that are involved in the sequential ... Read more >>

Med Chem (Medicinal chemistry (Shariqah (United Arab Emirates)))
[2020, 16(5):689-702]

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Exploration of quinolone and quinoline derivatives as potential anticancer agents.

Jamshed Iqbal, Syeda Abida Ejaz, Imtiaz Khan, Elina Ausekle, Mariia Miliutina, Peter Langer,

<h4>Background</h4>Among the different types of cancers, breast cancer, bone cancer and cervical cancer are the most common gender specific cancer types that are affecting the women worldwide. Currently, many enzymatic and cellular pathways are known as drug targets for the treatment of cancer. Even though many improvements have been made ... Read more >>

Daru (Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences)
[2019, 27(2):613-626]

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Rapid and Accurate Automatic Temperature Calibration of Disposable Screen-printed Heated Gold Electrodes

Sonivette Colón-Rodríguez, Martin Schönhoff, Juhaina Abdulkhalek, Tatiana Quiñones-Ruíz, Stephen Bentham, Gourav Bhowmik, Mengbing Huang, Peter Langer, Igor Lednev, Gerd-Uwe Flechsig,

Joule-heated electrodes have been used to enhance electrochemical analysis. Due to such direct heating, a steep temperature gradient is created near the electrode surface. The heating device that provides the high-frequency AC (50 kHz or more) has to be calibrated, in order to apply the desired temperature during analysis. The ... Read more >>

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Arterial stiffness and haemodynamic regulation in adolescent anorexia nervosa versus obesity.

Ingrid Tonhajzerova, Andrea Mestanikova, Alexander Jurko, Marian Grendar, Peter Langer, Igor Ondrejka, Tomas Jurko, Igor Hrtanek, Dana Cesnekova, Michal Mestanik,

Cardiovascular complications contribute to higher morbidity and mortality in patients with anorexia nervosa. We aimed to study biomarkers of cardiovascular risk in anorexic, normal-weight, and obese adolescents with focus on complex cardiovascular autonomic regulation and early arteriosclerotic damage. We examined 20 adolescent girls with anorexia nervosa, 20 obese girls, and ... Read more >>

Appl Physiol Nutr Metab (Applied physiology, nutrition, and metabolism = Physiologie appliquee, nutrition et metabolisme)
[2020, 45(1):81-90]

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Household Surveys in the General Population and Web-Based Surveys in IQOS Users Registered at the Philip Morris International IQOS User Database: Protocols on the Use of Tobacco- and Nicotine-Containing Products in Germany, Italy, and the United Kingdom (Greater London), 2018-2020.

Zheng Sponsiello-Wang, Peter Langer, Luis Prieto, Mariia Dobrynina, Dimitra Skiada, Nathalie Camille, Rolf Weitkunat, Frank Lüdicke,

<h4>Background</h4>Philip Morris International (PMI) has developed a novel heat-not-burn tobacco product, Tobacco Heating System (THS), which is marketed under the brand name of IQOS with HEETS (IQOS). The aerosol generated by THS has substantially fewer toxicants than combustible cigarette smoke, although the extent of the reduction of harmful and potentially ... Read more >>

JMIR Res Protoc (JMIR research protocols)
[2019, 8(5):e12061]

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Key Role of Reactive Oxygen Species (ROS) in Indirubin Derivative-Induced Cell Death in Cutaneous T-Cell Lymphoma Cells.

Marwa Y Soltan, Uly Sumarni, Chalid Assaf, Peter Langer, Ulrich Reidel, Jürgen Eberle,

Cutaneous T-cell lymphoma (CTCL) may develop a highly malignant phenotype in its late phase, and patients may profit from innovative therapies. The plant extract indirubin and its chemical derivatives represent new and promising antitumor strategies. This first report on the effects of an indirubin derivative in CTCL cells shows a ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2019, 20(5):]

Cited: 3 times

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Anti-proliferative Effects of Chromones: Potent Derivatives Affecting Cell Growth and Apoptosis in Breast, Bone-marrow and Cervical Cancer Cells.

Syeda Abida Ejaz, Mariia Miliutina, Peter Langer, Aamer Saeed, Jamshed Iqbal,

<h4>Background</h4>Previously, we have identified 3,3'-carbonyl-bis(chromones) (1a-h, 5e) and 3-(5-(benzylideneamino)thiozol-3-yl)-2H-chromen-2-ones (7a-j) as potent inhibitors of tissue non-specific alkaline phosphatase (TNAP). The present study was designed to investigate the cytotoxic and pro-apoptotic effect of the said derivatives.<h4>Methods</h4>The anti-proliferative effect of the derivatives was investigated in three cancer cell lines i.e., MCF-7, K-562, ... Read more >>

Med Chem (Medicinal chemistry (Shariqah (United Arab Emirates)))
[2019, 15(8):883-891]

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Crucial role of reactive oxygen species (ROS) for the proapoptotic effects of indirubin derivative DKP-073 in melanoma cells.

Veselina Zhivkova, Felix Kiecker, Peter Langer, Jürgen Eberle,

Melanoma represents a prime example demonstrating the success of targeted therapy in cancer. Nevertheless, it remained a deadly disease until now, and the identification of new, independent strategies as well as the understanding of their molecular mechanisms may help to finally overcome the high mortality. Both indirubins and TNF-related apoptosis-inducing ... Read more >>

Mol Carcinog (Molecular carcinogenesis)
[2019, 58(2):258-269]

Cited: 3 times

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One-Pot Synthesis of Dibenzo[ b, d]oxepines via Olefinic C-F Bond Functionalization and Intramolecular Pd-Catalyzed C-H Arylation.

Elina Ausekle, Peter Ehlers, Alexander Villinger, Peter Langer,

We report base-mediated reactions of 1-bromo-2-(2,2-difluorovinyl)benzenes with phenols followed by Pd-catalyzed intramolecular C-H arylation, which offers a novel route to a pharmaceutically relevant class of compounds, oxepines. Construction of these medium-sized ring structures proceeds as a one-pot two-step reaction through diaryl ketene acetals as intermediates. It allows to obtain various ... Read more >>

J Org Chem (The Journal of organic chemistry)
[2018, 83(22):14195-14202]

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Synthesis of furo[3,2-b:4,5-b']diindoles and their optical and electrochemical properties.

Huy Do Hoang, Julia Janke, Aneta Amirjanyan, Tariel Ghochikyan, Anika Flader, Alexander Villinger, Peter Ehlers, Stefan Lochbrunner, Annette-Enrica Surkus, Peter Langer,

An efficient two-step palladium catalyzed synthesis of furo[3,2-b:4,5-b']diindoles, a hitherto unknown symmetrical heterocyclic core structure, was developed. The synthesis is based on a regioselective Suzuki-Miyaura cross coupling reaction of tetrabromofuran and subsequent double N-arylation. Selected compounds were studied with regard to their optical and electrochemical properties. The compounds show fluorescence ... Read more >>

Org Biomol Chem (Organic & biomolecular chemistry)
[2018, 16(35):6543-6551]

Cited: 1 time

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Respiratory sinus arrhythmia - testing the method of choice for evaluation of cardiovagal regulation.

Michal Mestanik, Andrea Mestanikova, Peter Langer, Marian Grendar, Alexander Jurko, Nikola Sekaninova, Nadezda Visnovcova, Ingrid Tonhajzerova,

Respiratory sinus arrhythmia (RSA) is an index of cardiovagal regulation, emotional and cognitive processing. RSA is quantified using heart rate variability (HRV) spectral analysis at respiratory-linked high-frequency band (HF-HRV) using Fast Fourier transformation (FFT) or autoregressive (AR) method, both requiring resampling of recordings - a potential source of error. We ... Read more >>

Respir Physiol Neurobiol (Respiratory physiology & neurobiology)
[2019, 259:86-92]

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Thermal degradation behavior and X-ray diffraction studies of chitosan based polyurethane bio-nanocomposites using different diisocyanates.

Muhammad Asif Javaid, Muhammad Rizwan, Rasheed Ahmad Khera, Khalid Mahmood Zia, Kei Saito, Muhammad Zuber, Javed Iqbal, Peter Langer,

Five different samples of chitosan based polyurethane bio-nanocomposites (PUBNCs) were synthesized by step growth polymerization technique. Five different diisocyanates were used by keeping hydroxyl terminated polybutadiene (HTPB)/1,4-butane diol (1,4-BDO)/chitosan (CS) and montmorillonite (MMT) clay ratios constant (PUR1-PUR5). For comparative studies, PUR-6 was prepared without CS and clay components. Molecular characterizations ... Read more >>

Int J Biol Macromol (International journal of biological macromolecules)
[2018, 117:762-772]

Cited: 4 times

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Identification of New Chromenone Derivatives as Cholinesterase Inhibitors and Molecular Docking Studies.

Jamshed Iqbal, Muhammad S A Abbasi, Sumera Zaib, Saifullah Afridi, Norbert Furtmann, Jürgen Bajorath, Peter Langer,

<h4>Background</h4>Alzheimer's Disease (AD) is the leading cause of dementia among the aging population. This devastating disorder is generally associated with the gradual memory loss, specified by a decrease of acetylcholine level in the cortex hippocampus of the brain due to hyperactivation of cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)).<h4>Objective</h4>Therefore, inactivation of ... Read more >>

Med Chem (Medicinal chemistry (Shariqah (United Arab Emirates)))
[2018, 14(8):809-817]

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Improved assessment of arterial stiffness using corrected cardio-ankle vascular index (CAVI0) in overweight adolescents with white-coat and essential hypertension.

Michal Mestanik, Alexander Jurko, Bart Spronck, Alberto P Avolio, Mark Butlin, Tomas Jurko, Zuzana Visnovcova, Andrea Mestanikova, Peter Langer, Ingrid Tonhajzerova,

Arterial stiffness is a marker of vascular damage. Although adiposity increases cardiovascular risk, the relationship between paediatric overweight and arterial stiffness is unclear. The study aimed to evaluate the simultaneous effect of hypertension and overweight on arterial stiffness using cardio-ankle vascular index (CAVI) and related novel, theoretically blood pressure (BP)-independent, ... Read more >>

Scand J Clin Lab Invest (Scandinavian journal of clinical and laboratory investigation)
[2017, 77(8):665-672]

Cited: 4 times

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Pd-catalyzed coupling reactions of anhydro-aldose tosylhydrazones with aryl bromides to produce substituted exo-glycals.

Tímea Kaszás, Anton Ivanov, Marietta Tóth, Peter Ehlers, Peter Langer, László Somsák,

Palladium-catalyzed cross-couplings of O-peracylated and O-permethylated 2,6-anhydro-aldose tosylhydrazones with aryl halides were studied under thermic conditions in the presence of LiOtBu and phosphine ligands. The reactions gave the corresponding aryl substituted exo-glycals as mixtures of diastereomers in 11-75% yields. The transformations represent a new access to these types of glycomimetic ... Read more >>

Carbohydr Res (Carbohydrate research)
[2018, 466:30-38]

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Synthesis of Unsymmetrical Aza-Ullazines by Intramolecular Alkynyl-Carbonyl Metathesis.

Silvio Parpart, Sebastian Boldt, Peter Ehlers, Peter Langer,

A variety of aza-ullazines were synthesized in one step from readily accessible 3,5-dialkynyl-4-pyrrolopyridine via acylation followed by intramolecular alkynyl carbonyl metathesis. The reaction conditions were optimized, and the preparative scope was studied. The optoelectronic properties of selected aza-ullazines were studied by UV/vis and fluorescence spectroscopy. ... Read more >>

Org Lett (Organic letters)
[2018, 20(1):122-125]

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2-Substituted 7-trifluoromethyl-thiadiazolopyrimidones as alkaline phosphatase inhibitors. Synthesis, structure activity relationship and molecular docking study.

Behzad Jafari, Meirambek Ospanov, Syeda Abida Ejaz, Nazym Yelibayeva, Shafi Ullah Khan, Sayyeda Tayyeba Amjad, Sayfidin Safarov, Zharylkasyn A Abilov, Mirgul Zh Turmukhanova, Sergey N Kalugin, Peter Ehlers, Joanna Lecka, Jean Sévigny, Jamshed Iqbal, Peter Langer,

Alkaline Phosphatases (APs) play a key role in maintaining a ratio of phosphate to inorganic pyrophosphate (Pi/PPi) and thus regulate extracellular matrix calcification during bone formation and growth. Among different isozymes of AP, aberrant increase in the level of tissue non-specific alkaline phosphatase (TNAP) is strongly associated with vascular calcification ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 144:116-127]

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A domino reaction of 3-chlorochromones with aminoheterocycles. Synthesis of pyrazolopyridines and benzofuropyridines and their optical and ecto-5'-nucleotidase inhibitory effects.

Mariia Miliutina, Julia Janke, Sidra Hassan, Sumera Zaib, Jamshed Iqbal, Joanna Lecka, Jean Sévigny, Alexander Villinger, Aleksej Friedrich, Stefan Lochbrunner, Peter Langer,

A new and efficient domino reaction of 3-chlorochromones with electron-rich aminoheterocycles was developed which allows for a convenient synthesis of a variety of pyrazolo[3,4-b]pyridines, pyrrolo[2,3-b]pyridines, pyrido[2,3-d]pyrimidines and benzofuro[3,2-b]pyridines. The products exhibit strong fluorescence. In addition, they exhibit significant ecto-5'-nucleotidase inhibition properties and cytotoxic behavior. ... Read more >>

Org Biomol Chem (Organic & biomolecular chemistry)
[2018, 16(5):717-732]

Cited: 1 time

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Chemoselective synthesis and biological evaluation of arylated 2-(Trifluoromethyl) quinolines as nucleotide pyrophosphatase (NPPs) inhibitors.

David Kuhrt, Syeda Abida Ejaz, Saira Afzal, Shafi Ullah Khan, Joanna Lecka, Jean Sévigny, Peter Ehlers, Anke Spannenberg, Jamshed Iqbal, Peter Langer,

A new approach to arylated 2-trifluoromethylquinolines based on novel regioselective Suzuki-Miyaura coupling reactions has been developed. Moreover, site-selective, chemo-selective amination reactions were performed. The new 2-trifluoromethylquinoline derivatives were tested as potential NPPs inhibitors and evaluated for their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs and nucleoside triphosphate diphosphohydrolases ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 138:816-829]

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