Paclitaxel, carboplatin and gemcitabine combination as induction chemotherapy for stage IIIA N2 bulky non-small cell lung cancer

Background: Induct ion chemotherapy followed by surgical resection or definitive radiotherapy for patients affected by stage IIIA N2 bulky non-small cell lung cancer (NSCLC) has been investigated in several trials. Patients and Methods: In this present study, 52 patients with stage IIIA N2 bulky NSCLC with cytologically or histologically confirmed mediastinal lymph node involvement received paclitaxel 175 mg/mq on day 1, carboplatin AUC 5 on day 1 and gemcitabine 1,000 mg/mq on day 1 and 8 every 3 weeks for three cycles as induction chemotherapy. Results: Objective response (4 complete remission and 36 partial remission) was achieved in 40/52 patients. No early or toxic deaths were observed. Twenty-two patients were surgically explored. Fifteen were excluded for resection for biopsy-proven residual tumour in mediastinal nodes. Complete surgical resection was performed in 15 patients with confirmed pathological downstaging. Pathological complete response was achieved in 4 patients. No surgery-related mortality or significant morbidity was reported. Adjuvant radiotherapy was delivered in 15 patients, and 30 patients received definitive radiotherapy. Conclusion: In the present study, the combination of paclitaxel, carboplatin and gemcitabine has been a safe and active regimen in poor-prognosis stage IIIA N2 bulky NSCLC

Synthesis of a Small Library of Imidazolidin-2-ones using Gold Catalysis on Solid Phase

An efficient and high-yielding solid phase synthesis of a small library of imidazolidin-2-ones and imidazol-2-ones was carried out employing a high chemo- and regioselective gold-catalyzed cycloisomerization as a key step. Polymer-supported amino acids derivatized with several alkyne functionalities combined with tosyl- and phenylureas have been subjected to gold-catalysis exhibiting exclusively C–N bond formation. The present work proves the potential of solid phase synthesis and homogeneous gold catalysis as an efficient and powerful synthetic tool for the generation of drug-like heterocycles

Polymer-Supported Stereoselective Synthesis of Tetrahydrobenzopyrazino-thiadiazinone Dioxides via N-Sulfonyl Iminiums

The stereoselective synthesis of 1,2,11,11atetrahydrobenzo[e]pyrazino[1,2-b][1,2,4]thiadiazin-3(4H)- one 6,6-dioxides on a solid support via tandem N-sulfonyl iminium ion cyclization, followed by nucleophilic addition is reported. The synthesis proceeded with full control of stereoselectivity at the newly formed asymmetric carbon, under mild conditions, and using commercially available building blocks. The synthetic route provided high-purity crude productsFil: Cankarova, Nadezda. Palacký University; República ChecaFil: la Venia, Agustina. Palacký University; República Checa. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Krchnak, Viktor. Palacký University; República Checa. University of Notre Dame; Estados Unido

Palladium-Catalyzed Cross-Coupling Reactions of Arylsiloxanes with Aryl Halides: Application to Solid-Supported Organic Synthesis

The solid-phase version of the Pd-catalyzed Hiyama reaction between a variety of aryltriethoxysilanes and immobilized aryl halides was developed. Smooth crosscoupling was achieved to afford the corresponding biaryl products in moderate to excellent yields. The described protocol would be particularly useful for the construction of 4′-substituted 1,1′-biphenyl derivativesFil: Traficante, Carla Inés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; ArgentinaFil: Delpiccolo, Carina Maria Lujan. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; ArgentinaFil: Mata, Ernesto Gabino. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentin