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Dihydrofolate Reductase Inhibitors (dihydrofolate + reductase_inhibitor)
Selected AbstractsIn,vitro Effects of Plasmodium falciparum Dihydrofolate Reductase Inhibitors on Normal and Cancer Cell ProliferationCHEMMEDCHEM, Issue 3 2008Tiziana Rossi Prof. Toxicological evaluations were performed on two novel Plasmodium falciparum dihydrofolate reductase inhibitors and other known antimalarial drugs. Cytotoxicity tests were performed on Vero and MCF-7 cells and apoptotic and/or proliferative markers p21 and p53 and A, B1, D1, and D2 cyclines. The results are discussed and show that this molecule can be considered an interesting new candidate for further development. [source] Novel 2-hydrazino-pyrimidin-4(3H)-one derivatives as potential dihydrofolate reductase inhibitorsJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2010Mariam S. Degani Novel substituted 2-hydrazino-pyrimidin-4(3H)-one derivatives were synthesized and examined for their antifolate activity against DHFR from Pneumocystis carinii (pc), Toxoplasma gondii (tg), Mycobacterium avium (ma), and rat liver (rl). A novel, simple, and feasible methodology was developed for the synthesis of the titled compounds. Amongst these, compound 8 6-phenyl-2-(2-(1-(thiophen-2-yl) ethylidene)hydrazinyl) pyrimidin-4(3H)-one exhibited 17.74 ,M activity against pcDHFR. J. Heterocyclic Chem., (2010). [source] The use of folic acid antagonists and the risk of colorectal cancer,PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 10 2007Patricia F. Coogan Abstract Purpose Since folate is associated with a reduced risk of colorectal cancer, we hypothesized that folic acid antagonists might increase the risk. We used data from a population-based case control study of medication use and colorectal cancer to evaluate the hypothesis. Methods Case patients with adenocarcinoma of the colon or rectum were ascertained from participating hospitals in Massachusetts and the Massachusetts cancer registry (MCR) from January 1, 2001, through November 30, 2004. Age-, sex-, and precinct-matched control subjects were chosen from Massachusetts town lists. Information on folic acid antagonist use and other relevant data were obtained from 1809 cases and 1809 matched controls by telephone interview and by a self-administered dietary questionnaire. We used logistic regression models to estimate odds ratios among 1229 case patients and 1165 control subjects who provided satisfactory dietary information and did not have Crohn's disease or ulcerative colitis. Results The odds ratio for colorectal cancer among regular users of folate-containing supplements was 0.7 (95%CI 0.6,0.9). The odds ratio for regular use of folic acid antagonists was 1.3 (95%CI 0.9,1.9). Contrary to expectation, the odds ratio was reduced in the highest category of alcohol consumption (OR,=,0.5, 95%CI 0.2,1.2). The odds ratio was higher among users of drugs that inhibit dihydrofolate reductase (OR,=,1.6, 95%CI 0.9,2.8) than drugs that work through other mechanisms (OR,=,1.2, 95%CI 0.7,1.9). Conclusions Our data provide little support for the hypothesis that regular folic acid antagonist use increases the risk of colorectal cancer. However, there is a suggestion that dihydrofolate reductase inhibitors specifically may increase the risk. Copyright © 2007 John Wiley & Sons, Ltd. [source] In,vitro Effects of Plasmodium falciparum Dihydrofolate Reductase Inhibitors on Normal and Cancer Cell ProliferationCHEMMEDCHEM, Issue 3 2008Tiziana Rossi Prof. Toxicological evaluations were performed on two novel Plasmodium falciparum dihydrofolate reductase inhibitors and other known antimalarial drugs. Cytotoxicity tests were performed on Vero and MCF-7 cells and apoptotic and/or proliferative markers p21 and p53 and A, B1, D1, and D2 cyclines. The results are discussed and show that this molecule can be considered an interesting new candidate for further development. [source] | ||||||||||