OBJECTIVE To investigate the efficiency and safety of the oxaliplatin, fluorouracil （5-FU） and leucovorin regimen （FOLFOX）in previously untreated patients with metastatic or recurrent colorectal cancer. METHODS Pr...OBJECTIVE To investigate the efficiency and safety of the oxaliplatin, fluorouracil （5-FU） and leucovorin regimen （FOLFOX）in previously untreated patients with metastatic or recurrent colorectal cancer. METHODS Previously untreated patients with metastatic or recurrent colorectal cancer received 100 mg/m^2 of oxaliplatin intravenously （Ⅳ） over 2 h on day 1, and Ⅳ 400 mg/m^2 of leucovorin over 2 h followed by a bolus of 400 mg/m^2 of 5-FU. Then 2,600-3,000 mg/m^2 of 5-FU was administered by continuous infusion over 46 h. RESULTS An evaluated response rate was determined for 97 of 105 treated patients. The overall response rate was 35.1%, 9 patients （9.3%） had a complete response and 25 patients （25.8%） a partial response. Thirtytwo patients （33.0%） developed stable disease and 32.0% of the patients progressed. The median time to progression （TTP） was 7.7 months and the median overall survival 20.5 months. One and 2-year survival rates were 68% and 32%. Toxic effects based on the National Cancer Institute-Common Toxicity Criteria （NCI-CTC）, reaching grade 3/4 were： neutropenia 12.3%, anemia 11.3%, vomiting 4.1% and diarrhea 7.2%. Grade 3 neuropathy was 5.1%. The overall survival rate of patients who had received a radical resection was superior to the patients who had not received a operation, or had received a palliative resection （P=0.0658）. The serum levels of CEA, ALP and LDH had no relationship with survival （P〉0.05）. CONCLUSION The FOLFOX regimen containing oxaliplatin, 5-FU plus leucovorin was an efficacious regimen with good tolerability in previously untreated metastatic or recurrent colorectal cancer patients.展开更多
AIM： To compare ecabet sodium and cimetidine in relieving symptoms of functional dyspepsia. METHODS： We performed a multi-center, prospective, randomized, double-blinded controlled trial to compare the clinical effi...AIM： To compare ecabet sodium and cimetidine in relieving symptoms of functional dyspepsia. METHODS： We performed a multi-center, prospective, randomized, double-blinded controlled trial to compare the clinical efficacy of ecabet sodium and cimetidine in patients with functional dyspepsia. Two-hundred and seventy-two patients with dyspeptic symptoms fulfilling the Rome-II criteria were enrolled from 7 centers. In the study group （115 patients）, 1.5 g ecabet sodium was given twice a day. In the control group （121 patients）, 400 mg cimetidine was given twice a day. Symptoms and parameters of quality of life were analyzed at baseline, 3, 14, and 28 d after initiating the treatment. RESULTS： Two-hundred and thirty-six patients completed the clinical trial. After 4 wk of treatment, the rates of improvement in patients with dyspeptic symptoms were not different between two groups （77.4% in the ecabet group and 79.3% in the cimetidine group, respectively, P 〉 0.05）. Likewise, the rates of symptomatic improvement were not different at 3 d and 14 d. The parameters of quality of life did not change significantly during the study period in both groups. There was no clinically significant adverse event in both groups.展开更多
Fluvoxamine maleate is an excellent antidepressive drug. In the literatures, it was synthesized by the use of 4-（trifluoromethyl） aniline or 4-（trifluoromethyl） benzonitrile as starting materials and 5-methoxy-4＇...Fluvoxamine maleate is an excellent antidepressive drug. In the literatures, it was synthesized by the use of 4-（trifluoromethyl） aniline or 4-（trifluoromethyl） benzonitrile as starting materials and 5-methoxy-4＇-（trifluoromethyl-phenyl） valerophenone as a key intermediate. However, the methods in literatures have some disadvantages, such as the use of expensive materials, heavy pollution of environment, long reaction time and low yield of the product （only 30-40% overall yield）. We herein report an environmentally friendly synthetic method of fluvoxamine maleate, which used 4-（trifluoromethyl） benzoic acid and tetrahydrofuran as starting materials and FeCI3 as catalyst for the coupling of acid chloride with Grignard reagent. The fluvoxamine maleate was synthesized in 46% overall yield, through the oximation, etheration and salification of the intermediate successively.This method has some advantages, such as the use of commercially available materials, low cost, short production period （12-14 h）, high yield and light pollution.展开更多
A series of naphthalimide azoles as potential antibacterial and antifungal agents were conveniently and efficiently synthesized starting from commercially available 6-bromobenzo[de]isochromene-l,3-dione. All the new c...A series of naphthalimide azoles as potential antibacterial and antifungal agents were conveniently and efficiently synthesized starting from commercially available 6-bromobenzo[de]isochromene-l,3-dione. All the new compounds were characterized by NMR, IR, MS and HRMS spectra. Their antimicrobial activities were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi using two-fold serial dilution technique. The biological assay indicated that most of the prepared compounds exhibited inhibition to the tested strains. In particular, the triazolium derivatives not only gave higher ef- ficacy than their corresponding precursory azoles, but also demonstrated comparable or even better potency than the reference drugs Chloromycin, Orbifloxacin and Fluconazole. Some factors including structural fragments, pH and ClogP values of the target molecules were also preliminarily discussed.展开更多
文摘OBJECTIVE To investigate the efficiency and safety of the oxaliplatin, fluorouracil （5-FU） and leucovorin regimen （FOLFOX）in previously untreated patients with metastatic or recurrent colorectal cancer. METHODS Previously untreated patients with metastatic or recurrent colorectal cancer received 100 mg/m^2 of oxaliplatin intravenously （Ⅳ） over 2 h on day 1, and Ⅳ 400 mg/m^2 of leucovorin over 2 h followed by a bolus of 400 mg/m^2 of 5-FU. Then 2,600-3,000 mg/m^2 of 5-FU was administered by continuous infusion over 46 h. RESULTS An evaluated response rate was determined for 97 of 105 treated patients. The overall response rate was 35.1%, 9 patients （9.3%） had a complete response and 25 patients （25.8%） a partial response. Thirtytwo patients （33.0%） developed stable disease and 32.0% of the patients progressed. The median time to progression （TTP） was 7.7 months and the median overall survival 20.5 months. One and 2-year survival rates were 68% and 32%. Toxic effects based on the National Cancer Institute-Common Toxicity Criteria （NCI-CTC）, reaching grade 3/4 were： neutropenia 12.3%, anemia 11.3%, vomiting 4.1% and diarrhea 7.2%. Grade 3 neuropathy was 5.1%. The overall survival rate of patients who had received a radical resection was superior to the patients who had not received a operation, or had received a palliative resection （P=0.0658）. The serum levels of CEA, ALP and LDH had no relationship with survival （P〉0.05）. CONCLUSION The FOLFOX regimen containing oxaliplatin, 5-FU plus leucovorin was an efficacious regimen with good tolerability in previously untreated metastatic or recurrent colorectal cancer patients.
文摘AIM： To compare ecabet sodium and cimetidine in relieving symptoms of functional dyspepsia. METHODS： We performed a multi-center, prospective, randomized, double-blinded controlled trial to compare the clinical efficacy of ecabet sodium and cimetidine in patients with functional dyspepsia. Two-hundred and seventy-two patients with dyspeptic symptoms fulfilling the Rome-II criteria were enrolled from 7 centers. In the study group （115 patients）, 1.5 g ecabet sodium was given twice a day. In the control group （121 patients）, 400 mg cimetidine was given twice a day. Symptoms and parameters of quality of life were analyzed at baseline, 3, 14, and 28 d after initiating the treatment. RESULTS： Two-hundred and thirty-six patients completed the clinical trial. After 4 wk of treatment, the rates of improvement in patients with dyspeptic symptoms were not different between two groups （77.4% in the ecabet group and 79.3% in the cimetidine group, respectively, P 〉 0.05）. Likewise, the rates of symptomatic improvement were not different at 3 d and 14 d. The parameters of quality of life did not change significantly during the study period in both groups. There was no clinically significant adverse event in both groups.
文摘Fluvoxamine maleate is an excellent antidepressive drug. In the literatures, it was synthesized by the use of 4-（trifluoromethyl） aniline or 4-（trifluoromethyl） benzonitrile as starting materials and 5-methoxy-4＇-（trifluoromethyl-phenyl） valerophenone as a key intermediate. However, the methods in literatures have some disadvantages, such as the use of expensive materials, heavy pollution of environment, long reaction time and low yield of the product （only 30-40% overall yield）. We herein report an environmentally friendly synthetic method of fluvoxamine maleate, which used 4-（trifluoromethyl） benzoic acid and tetrahydrofuran as starting materials and FeCI3 as catalyst for the coupling of acid chloride with Grignard reagent. The fluvoxamine maleate was synthesized in 46% overall yield, through the oximation, etheration and salification of the intermediate successively.This method has some advantages, such as the use of commercially available materials, low cost, short production period （12-14 h）, high yield and light pollution.
基金partially supported by National Natural Science Foundation of China [21172181, 81250110089, 81250110554 (The Research Fellowship for International Young Scientists from International (Regional) Cooperation and Exchange Program)]the key program from Natural Science Foundation of Chongqing (CSTC2012jjB10026)+1 种基金the Specialized Research Fund for the Doctoral Program of Higher Education of China (SRFDP 20110182110007)the Fundamental Research Funds for the Central Universities (the key program XDJK2012B026)
文摘A series of naphthalimide azoles as potential antibacterial and antifungal agents were conveniently and efficiently synthesized starting from commercially available 6-bromobenzo[de]isochromene-l,3-dione. All the new compounds were characterized by NMR, IR, MS and HRMS spectra. Their antimicrobial activities were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi using two-fold serial dilution technique. The biological assay indicated that most of the prepared compounds exhibited inhibition to the tested strains. In particular, the triazolium derivatives not only gave higher ef- ficacy than their corresponding precursory azoles, but also demonstrated comparable or even better potency than the reference drugs Chloromycin, Orbifloxacin and Fluconazole. Some factors including structural fragments, pH and ClogP values of the target molecules were also preliminarily discussed.
