- Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice
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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.
- Jung, Soo Yeon,Lee, So Hyung,Kang, Han Byul,Park, Hang Ah,Chang, Sun Ki,Kim, Jungahn,Choo, Dong Joon,Oh, Chun Rim,Kim, Young Deuk,Seo, Ji Hyung,Lee, Kyung-Tae,Lee, Jae Yeol
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Read Online
- Quinolines from Morita-Baylis-Hillman acetates of 2-azidobenzaldehydes
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A simple method for synthesizing several 2-alkoxy-3-arylsulfinylmethylquinolines using an aza-Wittig type reaction of 3-(2-azidophenyl)-2-(arylsulfinylmethyl)propenoates, which were readily obtained from the Morita-Baylis-Hillman acetates of 2-azidobenzal
- Han, Eun-Gu,Kim, Hea Jung,Lee, Kee-Jung
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experimental part
p. 9616 - 9625
(2010/02/27)
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- 3,4-DIHYDROQUINAZOLINE DERIVATIVES
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The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity.
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- Synthesis and SAR study of T-type calcium channel blockers. Part II
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3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R 1, a biphenyl group at R2, and a benzyl amido group at R3 in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090).
- Yun, Jeong Choe,Han, Na Seo,Soo, Yeon Jung,Rhim, Hyewhon,Kim, Jungahn,Dong, Joon Choo,Jae, Yeol Lee
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scheme or table
p. 661 - 664
(2009/04/07)
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- 2-(3-Phenyl-2-piperazinyl-3,4-dihydroquinazolin-4-yl)acetic acids as antiviral agents, especially against cytomegaloviruses
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The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.
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- Discovery of potent T-type calcium channel blocker
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The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC50 = 41 ± 1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.
- Seo, Han Na,Choi, Ja Youn,Choe, Yun Jeong,Kim, Yoonjee,Rhim, Hyewhon,Lee, So Ha,Kim, Jungahn,Joo, Dong Jun,Lee, Jae Yeol
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p. 5740 - 5743
(2008/03/11)
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- Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers
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We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca2+ channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca2+ channels and N-type Ca2+ chann
- Rhim, Hyewhon,Lee, Yong Sup,Park, Seong Jun,Chung, Bong Young,Lee, Jae Yeol
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p. 283 - 286
(2007/10/03)
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- 2-(3-PHENYL-2-PIPERAZINYL-3,4-DIHYDROQUINAZOLINE-4-YL) ACETIC ACIDS AS ANTI-VIRAL AGENTS, ESPECIALLY AGAINST CYTOMEGALO VIRUSES
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The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.
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Page/Page column 18-19
(2008/06/13)
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