- Synthesis and in-vitro anti-hepatitis-B virus activity of 6H-[1]benzothiopyrano[4,3-b] quinolin-10-ols
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A series of 9-methoxy-6H-[1]benzothiopyrano[4,3-b]quinolin-10-ols with a Mannich side chain were synthesized and evaluated for their anti-Hepatitis B virus (HBV) activity in HepG2.2.15 cells. Some compounds showed significant anti-HBV activity with IC50 values less than 41 μM. Among them, compound 9b was the most effective anti-HBV agent (IC50 = 1.7 μM, SI = 60.3).
- Jia, Wei,Zhao, Yanfang,Li, Rongdong,Wu, Yanjiao,Li, Zebiao,Gong, Ping
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scheme or table
p. 507 - 512
(2009/12/06)
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- Synthesis and anti-HBV activities evaluation of new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives in vitro
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Some new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives have been synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a, 11b, 11c, 12c, 13c, 11g, and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC50 = 12.6 μM, SI = 12.4), 12c (IC50 = 3.5 μM, SI = 37.9), and 12g (IC50 = 2.6 μM, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC50 = 343.2 μM, SI = 7.0).
- Liu, Yajing,Zhao, Yanfang,Zhai, Xin,Liu, Xiuping,Sun, Lixue,Ren, Yanxia,Gong, Ping
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experimental part
p. 446 - 452
(2009/04/11)
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- Cleavage of the Methylenedioxy Ring. III. Cleavage with Sodium Benzyloxide in Dimethyl Sulfoxide
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Cleavage of the methylenedioxy ring in aromatic formyl (1-3), nitro (4 and 5), and acetyl (30) compounds with N-sodium benzyloxide-benzyl alcohol in dimethyl sulfoxide gave 3-hydroxybenzene derivatives (19, 22-24, 26, 27, and 33).In the case of the acetyl compound 30, the 4-hydroxybenzene derivative (34) was also obtained as a minor product.Regioselective cleavage of the ring in aromatic compounds having electronwithdrawing groups with nucleophilic oxide anions is discussed.Cleavage of the ring in 1-5 and 30 with 2 N sodium methoxide in dimethyl sulfoxide-dimethylformamide was found to be useful for the practical preparation of 3-hydroxybenzene derivatives (6-10 and 31).Keywords - Cleavage of methylenedioxy ring; regioselectivity; piperonals; 3,4-methylenedioxy-nitrobenzene; 3,4-methylenedioxy-acetophenone; sodium methoxide; sodium phenoxide; sodium benzyloxide; dimethyl sulfoxide; dimethylformamide
- Kobayashi, Shigeru,Okimoto, Kazuto,Imakura, Yasuhiro
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p. 1567 - 1573
(2007/10/02)
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