Efficacy of docetaxel combined with oxaliplatin and fluorouracil against stage Ⅲ/Ⅳ gastric cancer

AIM:To investigate the clinical efficacy and toxic effects of neoadjuvant chemotherapy using docetaxel combined with oxaliplatin and fluorouracil for treating stageⅢ/Ⅳgastric cancer.METHODS:A total of 53 stageⅢ/Ⅳgastric cancer patients were enrolled into the study and treated with neoadjuvant chemotherapy.Two of the cases were excluded.The program was as follows:75 mg/m2docetaxel and 85 mg/m2 oxaliplatin on day 1 and 1500mg/m2 fluorouracil on days 1 to 3 for three weeks.RESULTS:The tumour changes,postoperative remission rate,changes in the symptoms and adverse reactions were observed.The overall clinical efficacy(com-plete remission+partial remission)of the neoadjuvant chemotherapy was 62.7%.R0 radical resection was performed on 60.8%of the patients,with a remission rate(pathological complete response+pathological subtotal response+pathological partial response)of74.2%.The Karnofksy score improved in 42 cases.The toxicity reactions mostly included myelosuppression,followed by gastrointestinal mucosal lesions,nausea,vomiting and diarrhoea.CONCLUSION:Neoadjuvant chemotherapy consisting of docetaxel combined with oxaliplatin and fluorouracil is effective for stageⅢ/Ⅳgastric cancer.However,the treatment is associated with a high incidence of bone marrow suppression,which should be managed clinically.

Synthesis and in vitro biological evaluation of nitric oxide-releasing derivatives of hydroxylcinnamic acids as anti-tumor agents

Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil（5-FU） in most cancer cells tested.Furthermore,6f could selectively inhibit tumor cells,but not non-tumor cell proliferation.This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.

Design, synthesis, and biological evaluation of N-hydroxycinnamamide/salicylic acid hybrids as histone deacetylase inhibitors

Novel histone deacetylase （HDAC） inhibitors 9a-1 were designed and synthesized by coupling the carboxyl group of salicylic acid （SA） with N-hydroxycinnamamides through various alkylol amines, and their in vitro biological activities were evaluated. The N-hydroxycinnamamide/SA hybrids 9b-f and 9h showed good to moderate anti-tumor activities. Notably, compound 9e had a greater potency, comparable to vorinostat （SAHA）, in human colon carcinoma cells, which was probably, or at least partially, attributable to the positive effects of the chain length noted in allojlol amines. Furthermore, the HDAC inhibitory activities of 9e against Hela cell nuclear were also similar to that of vorinostat （SAHA）, while the tested compounds 9c-f did not exhibit any isoform selectivity in the inhibition of HDACs. In addition, compound 9e could selectively inhibit tumor cells, but not inhibit non-tumor cell proliferation in vitro. Our findings suggest that the N-hydroxycinnamamide/SA hybrids may hold significant promise as therapeutic a^ents for the intervention of human cancers.