[Short-term efficacy of intensity-modulated radiotherapy on esophageal carcinoma].

BACKGROUND AND OBJECTIVE: Intensity-modulated radiotherapy (IMRT) for esophageal carcinoma has seldom been reported; its clinical efficacy and toxicity are still uncertain. This study was to evaluate the short-term efficacy of IMRT on esophageal carcinoma, and to observe adverse events. METHODS: From June 2006 to March 2008, 37 patients with cervical and thoracic esophageal carcinoma were treated with IMRT. The treatment response, local control and survival were evaluated and the adverse events were observed. RESULTS: The minimal prescription dose of 100% of gross tumor volume (GTV D100) 95% of clinical target volume (CTV D95), and 95% of planning target volume (PTV D95) were (6 456+/-172)cGy, (6 293+/-145)cGy, and (5 988+/-53)cGy, respectively. The volumes of lung receiving irradiation of >or= 5 Gy, >or=10 Gy, >or=20 Gy and >or=30 Gy were (59.6+/-12.8)%, (39.5+/-8.7)%, (22.0+/-5.4)%, and (12.0+/-4.3)%, respectively. The mean lung dose (MLD) was (1 178+/-248)cGy. The overall response rate was 97.3% (36/37). The patients were followed-up for 8-29 months (median,13 months). The occurrence rates of grades 3-4 acute and late esophagitis, grades 2-4 acute and late pneumonitis were 16.2% and 7.2%, 10.8% and 8.1%. The 1-and 2-year local control rates were 72.9% and 72.9%. The 1-and 2-year overall survival rates were 80.9% and 67.4%. The 1-and 2-year disease-free survival rates were 73.5% and 51.4%. Local recurrence (69.2%) was the main reason of treatment failure. CONCLUSION: IMRT is an effective treatment for esophageal carcinoma with low occurrence of acute and late radiation-related pneumonitis, but local failure is still a main problem for treatment of patients with esophageal carcinoma.

Synthesis of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles as potential anticonvulsant agents.

A series of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles were synthesized. The anticonvulsant effect and neurotoxicity of the compounds (intraperitoneally) were evaluated with the maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc-PTZ), and rotarod tests in mice. 2-Phenyl-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3g) was the most active and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED(50)) of 29.5 mg/kg, a median toxicity dose (TD(50)) of 285 mg/kg, and a protective index (PI) of 9.7, which is greater than the reference drug, carbamazepine, which has a PI of 6.4.

Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity.

A series of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives were synthesized using 4-hydroxyquinolin-2(1H)-one as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and their neurotoxicities were measured by the rotarod test. The results of these tests demonstrated that 5-hexyloxy-[1,2,4]triazolo[4,3-a]quinoline (3f) was the most potent anticonvulsant, with median effective dose (ED(50)) of 19.0mg/kg and protective index (PI=TD(50)/ED(50)) values of 5.8 in the MES test. Compound 5-benzyloxy-[1,2,4]triazolo[4,3-a]quinoline (3j), exhibited a little weaker activity than compound 3f in controlling the seizure induced by MES test at the dose of 22.8 mg/kg, but it possessed lower neurotoxicity with PI value of 12.0, which was safer than marketed drug carbamazepine. To explain the possible mechanism of anticonvulsant activity, compound 3j was tested in pentylenetetrazole test, isoniazid test, thiosemicarbazide test, 3-mercaptopropionic acid and strychnine test.