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Pohang, South Korea

Moon J.T.,Korea Basic Science Institute | Ha S.H.,Korea Basic Science Institute | Lee S.H.,Korea Basic Science Institute | Kwon T.H.,Korea Basic Science Institute | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

First total synthesis of methylgerambullone (MGB, 1) isolated from Glycosmis angustifolia was completed via a convergent route. The effect of MGB on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine was investigated. As a result, it showed a potent relaxation rate (78.66 ± 4.30% at 100 mg/L) in a concentration-dependent manner on longitudinal smooth muscle contraction of isolated guinea-pig ileum induced by 1 μM acetylcholine. © 2009 Elsevier Ltd. All rights reserved. Source


Jung S.Y.,Kyung Hee University | Lee S.H.,Kyung Hee University | Kang H.B.,Kyung Hee University | Park H.A.,Kyung Hee University | And 8 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed. © 2010 Elsevier Ltd. All rights reserved. Source


Park H.A.,Kyung Hee University | Jung S.Y.,Kyung Hee University | Lee S.H.,Kyung Hee University | Kang H.B.,Kyung Hee University | And 7 more authors.
Bulletin of the Korean Chemical Society | Year: 2010

3,4-Dihydroquinazoline 1 as T-type calcium channel blocker was in vivo evaluated against A549 xenograft in BALB/c-nu Slc mice, which exhibited 54% tumor growth inhibition through oral administration of 8 mg/kg of body weight and was slightly less active than doxorubicin (68%). In addition, this compound was also profiled for its acute toxicity to ICR mice to afford oral LD50 value of 1,038 mg/kg of body weight. Source

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