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Dharmarajan Sriram Ruth Vandana Devakaram Murugesan Dinakaran Perumal Yogeeswari 《Medicinal chemistry research》2010,19(6):524-532
Nine orally active novel artemisinin derivatives were prepared from artemisinin by four-step synthesis, and the compounds
were evaluated in the rodent model using multidrug resistant Plasmodium yoelii nigeriensis. All of the compounds exhibited antimalarial activities with the ED50 ranging from 5.41 mg/kg–12.4 mg/kg. Among them, artemisinin derivative bearing N-(4-hydroxy-3-((4-phenylpiperazin-1-yl)methyl)phenyl)
moiety (5f) was found to be the most active compound and was found to be three times more potent than artemisinin (ED50 16.4 mg/kg). 相似文献
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Murugesan G Jeffrey R Amey CG Deane FP Kelly B Stain H 《The Australian and New Zealand journal of psychiatry》2007,41(4):343-350
OBJECTIVE: The aim of the present study was to describe an inpatient psychosocial rehabilitation programme in rural New South Wales and to assess the effectiveness of the programme using measures of clinically significant change. METHOD: The first 88 patients with a schizophrenia spectrum disorder to enter the Manara Clinic and Turon House, New South Wales, psychosocial rehabilitation programmes were assessed at admission and discharge using the Brief Psychiatric Rating Scale, the Health of the Nation Outcome Scales, and the Kessler-10 self-report measure. RESULTS: Significant improvements in psychiatric symptomatology, psychosocial functioning, and psychological distress were found over the course of the inpatient stay. Clinical significance analyses using patients in the community as the reference group indicated a reliable and clinically significant improvement for 33% of inpatients on psychiatric symptomatology, 39% of inpatients on psychosocial functioning, and 21% of inpatients on psychological distress. CONCLUSIONS: The psychosocial rehabilitation programme provides clinically significant initial benefits for patients with severe mental illnesses. More attention needs to be paid to evaluating which components of psychosocial rehabilitation contribute most to these benefits. Follow-up evaluation is required to determine whether the benefits of this programme are sustained in the community. 相似文献
45.
Curcumin induces G2/M arrest and apoptosis in cisplatin-resistant human ovarian cancer cells by modulating Akt and p38 MAPK 总被引:3,自引:0,他引:3
Weir NM Selvendiran K Kutala VK Tong L Vishwanath S Rajaram M Tridandapani S Anant S Kuppusamy P 《Cancer biology & therapy》2007,6(2):178-184
Curcumin, a major active component of turmeric, is known to induce apoptosis in several types of cancer cells, but little is known about its activity in chemoresistant cells. Hence, the aim of the present study was to investigate the anticancer properties of curcumin in cisplatin-resistant human ovarian cancer cells in vitro. The results indicated that curcumin inhibited the proliferation of both cisplatin-resistant (CR) and sensitive (CS) human ovarian cancer cells almost equally. Enhanced superoxide generation was observed in both CR and CS cells treated with curcumin. Curcumin induced G(2)/M phase cell-cycle arrest in CR cells by enhancing the p53 phosphorylation and apoptosis through the activation of caspase-3 followed by PARP degradation. Curcumin also inhibited the phosphorylation of Akt while the phosphorylation of p38 MAPK was enhanced. In summary, our results showed that curcumin inhibits the proliferation of cisplatin-resistant ovarian cancer cells through the induction of superoxide generation, G(2)/M arrest, and apoptosis. 相似文献
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Sriram D Senthilkumar P Dinakaran M Yogeeswari P China A Nagaraja V 《Journal of medicinal chemistry》2007,50(24):6232-6239
Fifty-one 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro-6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acids were synthesized and evaluated for antimycobacterial in vitro and in vivo against Mycobacterium tuberculosis H37Rv (MTB), multi-drug-resistant Mycobacterium tuberculosis (MDR-TB) and Mycobacterium smegmatis (MC2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from M. smegmatis. Among the synthesized compounds, 1-tert-butyl-1,4-dihydro-7-(4,4-dimethyloxazolidin-3-yl)-6-nitro-4-oxo-1,8-naphthyridine-3-carboxylic acid (10q) was found to be the most active compound in vitro with an MIC of 0.1 microM against MTB and MDR-TB and was 3 and 455 times more potent than isoniazid against MTB and MDR-TB, respectively. In the in vivo animal model 10q decreased the bacterial load in lung and spleen tissues with 2.39 and 3.89-log10protections respectively at the dose of 50 mg/kg body weight. 相似文献
50.
Is adjuvant chemotherapy for bladder cancer safer in patients with an ileal conduit than a neobladder? 总被引:1,自引:0,他引:1
OBJECTIVE: To assess the safety of adjuvant chemotherapy in patients with neobladder reconstruction in comparison to ileal conduit, as radical cystectomy and urinary diversion is an effective curative surgical treatment for muscle-invasive and high-risk superficial bladder cancer, and adjuvant chemotherapy is usually considered for patients with clinical stage > T2 and nodal metastasis. PATIENTS AND METHODS: We analysed retrospectively patients who had had a radical cystectomy and urinary diversion between 1992 and 2004. Patients with high-risk disease who had adjuvant chemotherapy were identified and stratified based on the type of urinary diversion (ileal conduit or neobladder). The chemotherapy regimen, complications from the adjuvant chemotherapy and other relevant data were analysed. RESULTS: Overall, 343 patients had radical cystectomy, 40 had adjuvant chemotherapy; 25 had an ileal conduit and 15 had a neobladder. Patient characteristics including age, stage and follow-up were similar. In all, 55% of patients had grade 1 toxicity, 23% grade 2, 18% grade 3, and 13% grade 4. No patients had serious organ toxicity and none died. There were no significant differences in the toxicity among the two groups. CONCLUSIONS: Adjuvant chemotherapy appears to be safe in patients with a neobladder and equally safe in patients with an ileal conduit. Hence neobladder reconstruction should not be denied to patients with bladder cancer who are at high risk of recurrence and who might require adjuvant chemotherapy. 相似文献