geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin


, : Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin. European Journal of Medicinal Chemistry 47(1): 255-260

A series of conjugates of 5-Fluorouracil (5-FU) and emodin were synthesized by coupling trimethyl emodin with N(1), N(3) dialkylated 5-FU. The 5-FU moiety contained various substituents at the N(3)-position were linked to the 2-position of trimethyl emodin via a methylene linkage. Their cytotoxicity against three cancer cell lines and one noncancerous cell were studied. The results revealed that some of conjugates exhibited better or comparable in vitro antitumor activity to 5-FU and emodin and low toxicity in the normal cell. The structure-activity relationship study showed N(3)-aromatic substituent was important for their cytotoxic activity.

US$19.90

PMID: 22093761

DOI: 10.1016/j.ejmech.2011.10.050


Other references

Peter G.S.ooner; Mark C.M.rris, 2012: Long-term stock grazing management in Travelling Stock Reserves and influence on conservation values. We examined the nature of long-term grazing management implemented in 51 Travelling Stock Reserves (TSRs) in the Albury region, and investigated potential relationships between grazing intensity and conservation values. In general, grazing intensi...

Anonymous, 1991: Children of alcoholics. Recent Developments in Alcoholism 9: 1-359

Clément, N.; Patriarche, G.; Smaali, K.; Vaurette, Fçois.; Nishiguchi, K.; Troadec, D.; Fujiwara, A.; Vuillaume, D., 2012: Large array of sub-10-nm single-grain Au nanodots for use in nanotechnology. A uniform array of single-grain Au nanodots, as small as 5-8 nm, can be formed on silicon using e-beam lithography. The as-fabricated nanodots are amorphous, and thermal annealing converts them to pure Au single crystals covered with a thin SiO(2)...

Forman, J.B., 2001: Legal issues in cash balance pension plan conversions. Replacing a traditional pension with a cash balance plan raises a number of complicated and unsettled legal issues, including the protection of accrued benefits, the rate of benefit accrual, age discrimination and notice requirements. This article...

Ferraldeschi, R.; Arnedos, M.; Hadfield, K.D.; A'Hern, R.; Drury, S.; Wardley, A.; Howell, A.; Evans, D.Gareth.; Roberts, S.A.; Smith, I.; Newman, W.G.; Dowsett, M., 2012: Polymorphisms of CYP19A1 and response to aromatase inhibitors in metastatic breast cancer patients. Single nucleotide polymorphisms (SNPs) in the gene encoding aromatase (CYP19A1) have been associated with differential benefit from letrozole treatment in metastatic breast cancer (mBC) patients, but validation is lacking. The aim was to investiga...

McConell, G.K.; Costill, D.L.; Widrick, J.J.; Hickey, M.S.; Tanaka, H.; Gastin, P.B., 1993: Reduced training volume and intensity maintain aerobic capacity but not performance in distance runners. It has recently been shown that a 70% reduction in training volume, while maintaining training intensity, results in the maintenance of ovrhdot VO-2max and 5 km running performance in distance runners. The purpose of this study was to examine the...

John, G.T.; Punnoose, E.; Narasimhan, G.; Pulimood, B.M., 1994: Enhanced action of acenocoumarin in hyperthyroidism. Journal of the Association of Physicians of India 42(7): 575-575

Rogers, J.L.; Hunsaker, M.R.; Kesner, R.P., 2006: Effects of ventral and dorsal CA1 subregional lesions on trace fear conditioning. Recent lines of research have focused on dissociating function between the dorsal and ventral hippocampus along space and anxiety dimensions. In the dorsal hippocampus, the CA I subregion has been implicated in the acquisition of contextual fear a...

Skucas, J.; Gorski, J., 1975: New grid design for a fluoroscopic spot film device. A new grid design for a fluoroscopic spot film device is presented. Fluoroscopy is achieved with a conventional low ratio grid, while spot filming is done with a high ratio criss-cross grid. The result is a low patient radiation dose during fluoro...

Bannert, B.; Schobersberger, W.; Tran, U.; Remmel, A., 2011: The effectiveness of a nondiet multidisciplinary weight reduction program for severe overweight patients with psychological comorbidities. Objective. For successful sustainable weight reduction, a multimodal program including behaviour therapy is needed. Lifestyle modification is mostly used for obesity BMI <40 kg/m(2). The present study demonstrated the effect of an in-patient...