bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: A Study of Antibacterial Activity of Some Novel 8‐Methoxy‐4‐methyl‐quinoline Derivatives.
Authors: Singh Sheoraj , Kumar Vikas , Kumar Ashok , Sharma Shalabh , Dua Piyush 
Published: March 2011

AbstractNovel azetidinylamino‐ and thiazolidinylaminoquinolines are synthesized starting from quinolinol derivative (I), and evaluated in vitro for their antibacterial activity against gram positive bacteria.
ChemInform Abstract: Regioselective Introduction of Homoallylic Amine Moiety to Quinolines: Preparation of Reissert Compound Followed by In‐Mediated Allylation of Nitrile.
Authors: Kim Sung Hwan , Lee Sangku , Kim Yu Mi , Kim Jae Nyoung 
Published: March 2011

AbstractReissert compounds (I) are converted into homoallylic compounds (III) whereas the isoquinoline derived Reissert compound (IV) gives ring closure product (V) and N‐hexanoyl derivative (VI) unexpectedly yields imine (VII).
ChemInform Abstract: 4‐Hydroxy‐2‐quinolones. Part 179. Synthesis, Structure, and Antiinflammatory Activity of 4‐Hydroxy‐1‐methyl‐2‐oxo‐1,2‐dihydroquinolin‐3‐ylacetic Acid and Its Derivatives.
Authors: Ukrainets I. V. , Mospanova E. V. , Davidenko A. A. , Tkach A. A. , Gorokhova O. V. 
Published: March 2011

Abstract9 Esters of type (V) are prepared and screened for their anti‐inflammatory activities.
ChemInform Abstract: Conjugate Addition — SNAr Domino Reaction for the Synthesis of Benzo‐ or Pyridyl‐Fused Lactams and Sultams.
Authors: Noerager Niels Groen , Juhl Karsten 
Published: March 2011

AbstractThe synthesis is achieved via addition of deprotonated amides, sulfonamides or hydrazines to ethyl propiolate derivatives (II) followed by nucleophilic substitution.
ChemInform Abstract: 3‐Methoxalylchromone — A Versatile Reagent for the Regioselective Synthesis of 1‐Desazapurine.
Authors: Ostrovskyi Dmytro , Iaroshenko Viktor O. , Ali Iftikhar , Mkrtchyan Satenik , Villinger Alexander , Tolmachev Andrei , Langer Peter 
Published: March 2011

Abstract5‐Aminoimidazoles, prepared in situ from formimidate (II) and amines, react with title compound (I) to give the pharmaceutically important title skeleton (IV).
ChemInform Abstract: Synthesis of 2,3,4‐Tri‐Substituted 3,4‐Dihydroquinazolines via Tandem Nucleophilic Addition/Epoxy Ring‐Opening Cyclization Methodology Using N‐(2‐Oxiranylphenyl)carbodiimides with Nucleophiles.
Authors: Saito Takao , Ote Tatsuya , Shiotani Masahiro , Kataoka Hiroko , Otani Takashi , Kutsumura Noriki 
Published: March 2011

AbstractA variety of dihydroquinazolines are obtained diastereoselectively by reaction of carbodiimides (IX) with different O‐, S‐, N‐ and C‐nucleophiles.
ChemInform Abstract: Facile Synthesis of 1‐Methyl‐1H‐benzo[b]azepines from 1‐Methylquinolinium Iodides and Diazo(trimethylsilyl)methylmagnesium Bromide.
Authors: Morita Mikio , Hari Yoshiyuki , Aoyama Toyohiko 
Published: March 2011

AbstractStarting from iodide (I), the synthesis of benzoazepines (IV) is achieved via addition of magnesium salt (II), followed by sequential Cu‐catalyzed ring expansion and desilylation.
ChemInform Abstract: Interaction of Derivatives of 7‐Amino‐1,5‐benzodiazepin‐2‐ones with α,β‐Unsaturated Ketones.
Authors: Janciene R. , Stumbreviciute Z. , Vektariene A. , Sirutkaitis R. , Podeniene D. , Palaima A. , Puodziunaite B. 
Published: March 2011

AbstractDifferent products are obtained when diazepin‐2‐ones (I) or (VII) are reacted with α,β‐unsaturated carbonyl compounds (II) or (IV).
ChemInform Abstract: An Efficient Oxidative Dearomatization—Radical Cyclization Approach to Symmetrically Substituted Bicyclic Guttiferone Natural Products.
Authors: McGrath Nicholas A. , Binner Joshua R. , Markopoulos Georgios , Brichacek Matthew , Njardarson Jon T. 
Published: March 2011

AbstractThe core structure (VI) of guttiferone terpenes such as (VII) is prepared via a diacetoxyiodobenzene‐mediated oxidative dearomatization of phenol (II) and a subsequent radical cyclization of the resulting ketal as key steps.
ChemInform Abstract: Phenolic Constituents from the Galls of Pistacia integerrima Stewart
Authors: Ahmad Shamim , Ali Mohammed , Ansari Shahid H. 
Published: March 2011

Abstractisolation and characterization of pistiphloro‐glucinyl ester (I), pisticiphloroglucinyl ether (II) and pistaciaphenyl ether (III)
ChemInform Abstract: Asymmetric Total Synthesis of (+)‐Fumimycin via 1,2‐Addition to Ketimines.
Authors: Gross Patrick J. , Furche Filipp , Nieger Martin , Braese Stefan 
Published: March 2011

AbstractThe first total synthesis of (+)‐fumimycin, the unnatural enantiomer of the mycotoxin fumimycin, is accomplished.
ChemInform Abstract: Asymmetric Synthesis of the Natural erythro‐(1R,2S)‐8‐O‐4′‐Neolignan Myrislignan.
Authors: Xia Y. , Wang Wei 
Published: March 2011

AbstractThe synthesis of myrislignan (VI) is achieved in twelve steps from vanillin (I) with a total yield of 10% involving two key steps: preparation of the enantiopure threo alcohol (III) of predictable stereochemistry by dihydroxylation, and inversion of the absolute configuration at the C‐8 stereogenic center in (IV) to obtain the title compound with erythro configuration by a Mitsunobu reaction.
ChemInform Abstract: High‐Temperature and High‐Pressure Aqueous Solution Formation, Growth, Crystal Structure, and Magnetic Properties of BiFeO3 Nanocrystals.
Authors: Mi Jian‐Li , Jensen Thomas N. , Christensen Mogens , Tyrsted Christoffer , Joergensen Jens E. , Iversen Bo B. 
Published: March 2011

AbstractFormation and growth of the title nanocrystals in high‐temperature, high‐pressure aqueous KOH solutions of Fe(NO3)3 and Bi(NO3)3 is monitored by in situ synchrotron powder XRD.
ChemInform Abstract: Condensed Isoquinolines. Part 35. Synthesis and Reactions of 4H‐Thieno[3′,4′:5,6]pyrimido[1,2‐b]isoquinoline‐4,11(5H)‐dione.
Authors: Zadorozhny A. V. , Kovtunenko V. A. , Turov A. V. 
Published: March 2011

AbstractCompounds (I) are prepared by known methods.
ChemInform Abstract: Natural Products Containing Medium‐Sized Nitrogen Heterocycles Synthesized by Ring‐Closing Alkene Metathesis
Authors: van den Broek Sebastiaan A. M. W. , Meeuwissen Silvie A. , van Delft Floris L. , Rutjes Floris P. J. T. 
Published: March 2011

AbstractReview: 100 refs.
Wein zwischen Tradition und moderner Technik. Chemie und Genuss
Authors: Otteneder Herbert 
Published: March 2011

AbstractDie Grundschritte der Weinbereitung sind seit Jahrhunderten gleich geblieben. Geändert haben sich jedoch die technischen Mittel, die entscheidend zur Verbesserung der Weinqualität beigetragen haben. Trotz Reinzuchthefen, Stahltank, Einsatz von Eichenholzspänen, fraktionierter Destillation und einer ganzen Palette von Behandlungsmitteln findet vermehrt auch eine Rückbesinnung auf traditionelle Verfahren statt. An einzelnen Beispielen werden Für und Wider dieser Varianten dargestellt. Das vielfältige und weltweite Angebot der Weine haben auch zur Entwicklung einer ausgefeilten Analytik geführt. Dazu werden u.a. die Möglichkeiten der Authentizitätsprüfung mit Hilfe der Stabilisotopenanalytik aufgezeigt.
Unwiderstehlicher Hefeduft
Authors: Feil Sylvia 
Published: March 2011

AbstractFruchtfliegen (Drosopilidae) fliegen normalerweise keine Blüten zum Nektarsammeln an. Doch Aronstab‐Gewächse täuschen sie, um selbst bestäubt zu werden. Die Blüten ahmen den Duft überreifer Früchte nach, von denen sich Fruchtfliegen ernähren und in welche die Weibchen ihre Eier ablegen.
A phase 2 study of tasisulam sodium (LY573636 sodium) as second‐line treatment for patients with unresectable or metastatic melanoma
Authors: Kirkwood John M. , Gonzalez Rene , Reintgen Douglas , Clingan Philip R. , McWilliams Robert R. , de Alwis Dinesh P. , Zimmermann Annamaria , Brown Michael P. , Ilaria Robert L. , Millward Michael J. 
Published: March 2011

AbstractBACKGROUND:Tasisulam sodium (hereafter, tasisulam) is a novel anticancer agent that induces apoptosis through the intrinsic pathway and has antiangiogenic activity in preclinical models. Tasisulam demonstrated activity across a broad range of tumors, including melanoma. The primary objective of this phase 2 study was to determine the objective response rate (ORR) in patients who had received 1 previous systemic chemotherapy for unresectable/metastatic melanoma; secondary objectives were to evaluate the clinical response rate (CRR), progression‐free survival (PFS), overall survival (OS), duration of response, safety, and pharmacokinetics.METHODS:Tasisulam was administered intravenously on Day 1 of 21‐day cycles according to a lean body weight‐based dosing algorithm targeting a peak plasma concentration (Cmax) of 420 μg/mL.RESULTS:In 68 enrolled patients, the median age was 59 years (range, 26‐83 years). No patients had a complete response (CR), 8 patients had a partial response (PR), and 24 patients had stable disease (SD); the ORR (CR + PR) was 11.8%, and the CRR (CR + PR + SD) was 47.1%. The median PFS was 2.6 months, and the median OS was 9.6 months. The predominant treatment‐related grade 3/4 toxicity was thrombocytopenia (20.6% of patients). Tasisulam exhibited a biexponential disposition with a predicted distribution half‐life of 0.3 hours to 2.8 hours and a median terminal elimination half‐life of 10 days (consistent with the turnover of albumin), suggesting that tasisulam is very tightly bound to albumin.CONCLUSIONS:Tasisulam administered at a targeted Cmax of 420 μg/mL on Day 1 of 21‐day cycles demonstrated activity and tolerable toxicity as second‐line treatment in malignant melanoma. These results led to a registration trial in metastatic melanoma. Cancer 2011;. © 2011 American Cancer Society.
Impact of BRAF mutation and microsatellite instability on the pattern of metastatic spread and prognosis in metastatic colorectal cancer
Authors: Tran Ben , Kopetz Scott , Tie Jeanne , Gibbs Peter , Jiang Zhi‐Qin , Lieu Christopher H. , Agarwal Atin , Maru Dipen M. , Sieber Oliver , Desai Jayesh 
Published: March 2011

AbstractBACKGROUND:It is hypothesized that BRAF mutant cancers represent a discrete subset of metastatic colorectal cancer (CRC) defined by poorer survival. This study investigates whether BRAF mutant CRC is further defined by a distinct pattern of metastatic spread and explores the impact of BRAF mutation and microsatellite instability (MSI) on prognosis in metastatic CRC.METHODS:By using prospective clinical data and molecular analyses from 2 major centers (Royal Melbourne Hospital and The University of Texas MD Anderson Cancer Center), patients with known BRAF mutation status were analyzed for clinical characteristics, survival, and metastatic sites.RESULTS:The authors identified 524 metastatic CRC patients where BRAF mutation status was known; 57 (11%) were BRAF mutant tumors. BRAF mutant tumors were significantly associated with right‐sided primary tumor, MSI, and poorer survival (median, 10.4 months vs 34.7 months, P < .001). A distinct pattern of metastatic spread was observed in BRAF mutant tumors, namely higher rates of peritoneal metastases (46% vs 24%, P = .001), distant lymph node metastases (53% vs 38%, P = .008), and lower rates of lung metastases (35% vs 49%, P = .049). In additional survival analyses, MSI tumors had significantly poorer survival compared with microsatellite stable tumors (22.1 months vs 11.1 months, P = .017), but this difference was not evident in the BRAF mutant population.CONCLUSIONS:The pattern of metastatic spread observed in this study further defines BRAF mutant CRC as a discrete disease subset. The authors demonstrated that, unlikely early stage disease, MSI is associated with poorer survival in metastatic CRC, although this is driven by its association with BRAF mutation. Cancer 2011;. © 2011 American Cancer Society.
Nonmyeloablative allogeneic stem cell transplantation in relapsed/refractory chronic lymphocytic leukemia
Authors: Khouri Issa F. , Bassett Roland , Poindexter Nancy , O'Brien Susan , Bueso‐Ramos Carlos E. , Hsu Yvonne , Ferrajoli Alessandra , Keating Michael J. , Champlin Richard , Fernandez‐Vina Marcelo 
Published: March 2011

AbstractBACKGROUND:The role of nonmyeloablative allogeneic stem cell transplantation (NST) in the treatment of chronic lymphocytic leukemia (CLL) is not well established. The authors report on long‐term experience with NST in relapsed/refractory CLL and define prognostic factors associated with outcome.METHODS:The authors reviewed the outcome of 86 patients with relapsed/relapsed CLL enrolled in sequential NST protocols.RESULTS:The median patient age was 58 years. Patients were heavily pretreated before transplantation, and 43 required immunomanipulation after NST for persistent or recurrent disease. Immunomanipulation included withdrawal of immunosuppression, rituximab, and step‐wise donor lymphocyte infusions. Of 43 patients receiving immunomanipulation, 20 (47%) experienced a complete remission. Patients with human leukocyte antigen (HLA) genotype A1+/A2−/B44− were more likely to experience a complete remission (P = .0009), with rates of 9%, 36%, 50%, and 91%, respectively, for 0, 1, 2, and 3 of these HLA factors. This resulted in significant improvement in progression‐free‐survival rates of 68.2% at 5 years for patients with all 3 HLA factors. Overall, the estimated 5‐year survival rate was 51%. In a multivariate model, a CD4 count of <100/mm3 and a below normal serum immunoglobulin G level at study entry were associated with a short survival duration (P < .0001).CONCLUSIONS:These results confirm the potential cure of relapsed/refractory CLL with NST and provide the first evidence that immunoglobulin G and CD4 levels are predictive of overall survival after NST in CLL and that human leukocyte antigen alleles predict response to immunomanipulation. Cancer 2011;. © 2011 American Cancer Society.
Increasing accrual in cancer clinical trials with a focus on minority enrollment
Authors: Vicini Frank , Nancarrow‐Tull Joyce , Shah Chirag , Chmielewski Gary , Fakhouri Monty , Sitarek Stacey A. , Feczko Claire T. , Brzozowski Carol , Felten David L. 
Published: March 2011

AbstractBACKGROUND:The authors reviewed changes in accrual to cancer clinical trials over the last 2 decades at their institution with a focus on minority participation after the implementation of a community clinical oncology program (CCOP) and an aggressive, education‐orientated minority outreach program (MOP).METHODS:Data on patient enrollment in clinical trials for the years 1988 to 2010 was obtained from the William Beaumont Hospital (WBH) Cancer Clinical Trials Office. The type and number of cancers diagnosed and treated during the same period were obtained from the WBH tumor registry data. The MOP was initiated in the fall of 2003 with a focus on culture‐specific cancer education.RESULTS:With the development of the CCOP, clinical trials accrual increased significantly by 10‐fold (P = .001). The primary service area for the CCOP consistently averaged an 85% to 90% Caucasian population. During the same period, the minority population for the service area remained stable between 8.8% and 10% and did not change significantly. From 1999 to 2004, the WBH tumor registry data demonstrated that minorities represented 8.6% of cancers registered, whereas the average yearly minority enrollment from 2002 to 2004 was 5.4%. After initiation of the MOP, minority accrual doubled to 11% by 2010 with stable minority demographics.CONCLUSIONS:The current findings support the importance of a CCOP in supporting the accrual of patients to national clinical trials and increasing access to state‐of‐the art research. These data also strongly support focusing additional energy and educational efforts on targeting minority representation in clinical trials. Cancer 2011;. © 2011 American Cancer Society.
Phase 1 study of arsenic trioxide, high‐dose cytarabine, and idarubicin to down‐regulate constitutive signal transducer and activator of transcription 3 activity in patients aged <60 years with acute myeloid leukemia
Authors: Wetzler Meir , Andrews Chris , Ford Laurie A. , Tighe Sheila , Barcos Maurice , Sait Sheila N. J. , Block AnneMarie W. , Nowak Norma J. , Baer Maria R. , Wang Eunice S. , Baumann Heinz 
Published: March 2011

AbstractBACKGROUND:Constitutive activation of signal transducer and activator of transcription‐3 (STAT3) was detected in blasts from approximately 50% of patients with acute myeloid leukemia (AML) and was correlated with an adverse outcome. In vitro treatment of AML blasts with arsenic trioxide (ATO) down‐regulated STAT3 activity within 6 hours associated with a reduced viability within 48 hours.METHODS:A phase 1 clinical trial to evaluate the biologically effective dose and/or the maximally tolerated dose (MTD) of ATO in vivo in conjunction with high‐dose cytarabine (Hidac) and idarubicin (Ida) in patients with AML aged <60 years was conducted. Data were compared with 117 historic AML patients who had received treatment with Hidac/Ida.RESULTS:In total, 61 patients were enrolled onto 11 different dose levels (from 0.01 to 0.65 mg/kg ideal body weight). The MTD was 0.5 mg/kg. Compared with historic controls, patients who received ATO/Hidac/Ida, although they had similar pretreatment characteristics, had better overall survival (P = .039).CONCLUSIONS:ATO priming may have improved the outcome of patients aged <60 years with AML who received Hidac/Ida. The current data suggested that ATO may enhance the effect of chemotherapy. The authors concluded that further studies of this novel combination are warranted. Cancer 2011;. © 2011 American Cancer Society.
A phase 2 trial of complete resection for stage IV melanoma
Authors: Sosman Jeffrey A. , Moon James , Tuthill Ralph J. , Warneke James A. , Vetto John T. , Redman Bruce G. , Liu P. Y. , Unger Joseph M. , Flaherty Lawrence E. , Sondak Vernon K. 
Published: March 2011

AbstractBACKGROUND:On the basis of retrospective experience at individual centers, it appears that patients with stage IV melanoma who undergo complete resection have a favorable outcome compared with patients with disseminated stage IV disease. The Southwest Oncology Group (SWOG) performed a prospective trial in patients with metastatic melanoma who were enrolled before complete resection of their metastatic disease and provided prospective outcomes in the cooperative group setting.METHODS:Based on their physical examination and radiologic imaging studies, patients with a stage IV melanoma judged amenable to complete resection underwent surgery within 28 days of enrollment. All eligible patients were followed with scans (computed tomography or positron emission tomography) every 6 months until relapse and death.RESULTS:Seventy‐seven patients were enrolled from 18 different centers. Of those, 5 patients were ineligible; 2 had stage III disease alone; and 3 had no melanoma in their surgical specimen. In addition, 8 eligible patients had incompletely resected tumor. Therefore, the primary analysis included 64 completely resected patients. Twenty patients (31%) had visceral disease. With a median follow‐up of 5 years, the median relapse‐free survival was 5 months (95% CI, 3‐7 months) whereas median overall survival was 21 months (95% CI, 16‐34 months). Overall survivals at 3 and 4 years were 36% and 31%, respectively.CONCLUSIONS:In a prospective multicenter setting, appropriately selected patients with stage IV melanoma achieved prolonged overall survival after complete surgical resection. Although median relapse‐free survival was only 5 months, patients could still frequently undergo subsequent surgery for isolated recurrences. This patient population is appropriate for aggressive surgical therapy and for trials evaluating adjuvant therapy. Cancer 2011;. © 2011 American Cancer Society.
Phase 2 study of nilotinib as third‐line therapy for patients with gastrointestinal stromal tumor
Authors: Sawaki Akira , Nishida Toshirou , Doi Toshihiko , Yamada Yasuhide , Komatsu Yoshito , Kanda Tatsuo , Kakeji Yoshihiro , Onozawa Yusuke , Yamasaki Makoto , Ohtsu Atsushi 
Published: March 2011

AbstractBACKGROUND:Patients with gastrointestinal stromal tumors (GISTs) resistant to both imatinib and sunitinib have a poor prognosis and few therapeutic options. In this study, the efficacy and safety of nilotinib (AMN107) as a third‐line therapy for patients with GISTs was evaluated.METHODS:A single‐arm, open‐label trial was conducted in 8 Japanese hospitals. The key eligibility criteria included resistance or intolerance to both imatinib and sunitinib treatment. The primary endpoint was disease control rate, defined as the percentage of patients with complete response, partial response (PR), or stable disease (SD) lasting 24 weeks or longer.RESULTS:Thirty‐five patients were enrolled and treated with nilotinib 400 mg twice daily, which generally was well tolerated. Disease control rate at Week 24 was 29% (90% confidence interval, 16.4%‐43.6%). The median progression‐free survival was 113 days, and the median overall survival was 310 days. The objective response rate was 3%, comprising 1 PR in a patient with a GIST possessing both a KIT exon 11 mutation, and an imatinib‐resistant and sunitinib‐resistant KIT exon 17 mutation. Twenty‐three (66%) patients had SD (≥6 weeks) as the best response.CONCLUSIONS:These results suggest that nilotinib is generally well tolerated and has encouraging antitumor activity in patients with GIST who failed both imatinib and sunitinib. Cancer 2011;. © 2011 American Cancer Society.
Prognostic significance of baseline positron emission tomography and importance of clinical complete response in patients with esophageal or gastroesophageal junction cancer treated with definitive chemoradiotherapy
Authors: Suzuki Akihiro , Xiao Lianchun , Hayashi Yuki , Macapinlac Homer A. , Welsh James , Lin Steven H. , Lee Jeffrey H. , Bhutani Manoop S. , Maru Dipen M. , Hofstetter Wayne L. , Swisher Stephen G. , Ajani Jaffer A. 
Published: March 2011

AbstractBACKGROUND:Metabolic imaging is of interest in esophageal cancer; however, the usefulness of initial standardized uptake value (SUV) in positron emission tomography (PET) is unknown in patients with esophageal or gastroesophageal carcinoma treated with definitive chemoradiotherapy. The authors hypothesized that initial SUV would correlate with patient outcome.METHODS:The authors retrospectively analyzed esophageal or gastroesophageal carcinoma patients who had baseline PET and endoscopic ultrasonography in addition to other routine staging. All patients received definitive chemoradiotherapy. Multiple statistical methods were used.RESULTS:The authors analyzed 209 consecutive esophageal or gastroesophageal carcinoma patients treated with definitive chemoradiation for outcome; of these, 180 had baseline PET for additional analyses. The median overall survival (OS) for all patients was 20.7 months (95% confidence interval, 18.8‐26.3). Patients with clinical complete response (CR) lived longer than those with less than clinical CR (P < .0001). The median initial SUV was 12.7 (range, 0‐51). Higher initial SUV was associated with longer tumors (P = .0001), higher T‐stage status (P < .0001), positive N‐stage status (P = .0001), higher overall stage (P < .0001), lack of clinical CR (P = .0002), and squamous cell histology (P < .0001). In the univariate analysis, initial SUV was associated with OS (Cox model, P = .016; log‐rank test, P = .002). In the multivariate analysis, initial SUV dichotomized by the median value (P = .024) and tumor grade (P = .016) proved to be independent OS prognosticators. Median initial SUV for clinical CR patients was 10.2, compared with 15.3 for less than clinical CR patients (P = .0058).CONCLUSIONS:The data indicate that a higher initial SUV is associated with poorer OS in patients with esophageal or gastroesophageal carcinoma receiving definitive chemoradiation. Upon validation, baseline PET may become a useful stratification factor in randomized trials and for individualizing therapy. Cancer 2011;. © 2011 American Cancer Society.