Naphthofuroquinone derivatives: Inhibition of receptor tyrosine kinases

Lee, Kee‐In; Park, Youmie; Park, Su‐Jin; Hwang, Jung-Hwan; Lee, Sung‐Jin; Kim, Gun‐Do; Park, Woo‐Kyu; Lee, Sunghou; Jeong, Dae-Young; Kong, Jae-Yang; Kang, Hee‐Kyoung; Cho, Heeyeong

doi:10.1016/j.bmcl.2005.08.115

Cited by 21 publications

(6 citation statements)

References 16 publications

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“…20,21 Nitrofurantoin was initially administered for the eradication of what was then called Campylobacter pylori in 1988. 22 The furan ring raised much interest in medicinal chemistry: in the 1980s, the furan-based H2-histamine receptor blockers were synthesized leading to the highly successful ranitidine, 23 while the various furan compounds are being researched as anticancer, 24 antiviral 25 or anti-inflammatory 26 agents.…”

Section: Chemical and Microbiological Backgroundmentioning

confidence: 99%

Nitrofuran‐based regimens for the eradication of Helicobacter pylori infection

Buzás¹,

Józan

2007

J of Gastro and Hepatol

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Several aspects of Helicobacter pylori eradication have been meta-analyzed; however, nitrofuran-based therapies constitute an exception. The aim of this study was the systematic review and meta-analysis of the effect of furazolidone-and nitrofurantoin-based regimens in the eradication of infection. Studies evaluating the effects of nitrofurans on H. pylori were identified from Medline, EMBASE, the Cochrane Controlled Trials Register and congress abstracts. The studies were classified into groups based on first-, second-and third-line regimens. The pooled eradication rates and combined odd ratios of the individual studies were calculated and compared with the published meta-analysis. The factors influencing the efficiency of the regimens were also analyzed. Side-effects of nitrofuranbased regimens were also analyzed. The pooled eradication rate of primary proton pump inhibitor-based regimens containing furazolidone was 76.3% .2). The odds ratio for furazolidone-based regimens versus standard triple therapies was 2.34 (CI 0.76-3.92). Ranitidine bismuth citrate + furazolidone-based triple regimens were equally efficient (83.5%, CI 74.0-93.0, P = 0.06 versus triple therapies). Schedules including a H2 antagonist + furazolidone + one other antibiotic achieved pooled eradication rates of 79.9% (CI 67.8-89.9, P = 0.04). Bismuth-based triple therapies achieved 84.5% (CI 72.6-93.0, P = 0.002). Primary quadruple regimens containing furazolidone were superior to triple therapies (83.4%, CI 69.7-92.3, P = 0.01). Second-line schedules containing furazolidone obtained eradication rates of 76.1% (CI 66.4-85.0, P = 0.28 versus primary regimens). Third-line 'rescue' therapies were efficient in 65.5% of the cases (CI 56.3-75.5, P = 0.0001). Side-effects of the regimens containing furazolidone were more frequent than in standard therapies (P = 0.02). The combined odds ratio of side-effects for furazolidonebased versus standard therapies was 0.74 (CI 0.32-1.98). The duration of treatment, but not the furazolidone dose, influenced the treatment outcome. Primary triple regimens containing furazolidone are slightly less efficient than the standard primary combinations; primary quadruple regimens were more efficient than triple therapies. Furazolidone is also efficient as a component of second-line or rescue therapies.

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Section: Chemical and Microbiological Backgroundmentioning

confidence: 99%

Nitrofuran‐based regimens for the eradication of Helicobacter pylori infection

Buzás¹,

Józan

2007

J of Gastro and Hepatol

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“…However, in the case of the inhibitors of kinases, it is neither easy nor essential to get good selectivity for just one targeted kinase. Actually many inhibitors show cross-activities for several related kinases, which can also give benefi ts in the case of anticancer agents, since the simultaneous suppression of the activated signaling cascade by multiplex agents could synergistically act on the removal of tumors (Adams et al, 2002;Lee et al, 2006). As presented in Table 2, emodin showed little selectivity on RTKs; it repressed PDGFR-β, VEGFR-2, EGFR and FGFR-1 fairly well.…”

Section: Resultsmentioning

confidence: 99%

Screening of Kit inhibitors: suppression of Kit signaling and melanogenesis by emodin

Lee

Jeong

Park

et al. 2009

Phytotherapy Research

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In search of novel antipigmentation agents, a set of 3,840 compounds with natural-like synthetic or natural origin were screened against Kit (stem cell factor receptor). Emodin from the seed of Cassia tora and baicalin from Scutellariae radix showed potent inhibitory effects (IC(50) = 4.9 and 9.0 microM, respectively) on the phosphorylation of Kit. Emodin also blocked other receptor tyrosine kinase activities, such as epithelial growth factor receptor (EGFR), vascular endothelial growth factor receptor 2 (VEGFR-2), fibroblast growth factor receptor 1 (FGFR-1), platelet-derived growth factor receptor b (PDGFR-b). In contrast to emodin, aloe-emodin did not inhibit Kit activity at all. Emodin also blocked the cellular kinase activities of Kit and its down-stream p44/42 mitogen activated protein kinase (MAPK) in MO7e cells and human primary melanocytes. Emodin strongly suppressed the melanin synthesis triggered by stem cell factor (SCF) treatment. Also, emodin showed almost no toxicity up to 10 microM on cultured melanocytes as reported previously by other researchers. The results indicate that emodin is a good candidate for the development of antipigmentation agents since it can radically block the differentiation and proliferation of pigment cells by reducing Kit signaling.

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“…There are more than 100 papers related to the use of nitrofuran drugs for H. pylori treatment [9]. In fact, the furan compounds are also being researched as anticancer agents [12]. Similarly, bismuth compounds are still a part of the alternate therapies for patients who fail to respond to classical triple therapy and are considered safe and well-tolerated agents [13].…”

Section: Replymentioning

confidence: 99%