- BICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF
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The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s); R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); Xa and Xb are each C, N, O or S; Xc and Xd are each C or N; m is 0-2; n is 1-3; ring A is a 5-membered ring optionally having substituent(s); ring B is a 6-membered ring optionally having substituent(s); and ring C is a 3- to 5-membered ring optionally having substituent(s), provided that when Xa, Xc and Xd are each C, then Xb is N or S, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.
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Page/Page column 102-103
(2010/01/29)
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- Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles
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Four classes of UK-1 analogues were synthesized and their cytotoxicity testing against human A-549, BFTC-905, RD, MES-SA, and HeLa carcinoma cell lines was determined. The results revealed that UK-1 and four of these analogues (15-18) are potent against the cancer cell lines. In particular, compound 16 is more potent than UK-1 against A-549 and HeLa cell lines, and compounds 15, 17, and 18 selectively exhibit potent cytotoxic activity against the BFTV-905 cells (IC50 9.6 μM), A-549 cells (IC50 6.6 μM), and MES-SA cells (IC50 9.2 μM), respectively.
- Huang, Shu-Ting,Hsei, I-Jen,Chen, Chinpiao
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p. 6106 - 6119
(2007/10/03)
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- Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: Discovery and preliminary SAR of benzimidazole derivatives
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Benzimidazole 5-carboxamide derivatives from a combinatorial screening library were discovered as specific inhibitors of the NS5B polymerase of the hepatitis C virus (HCV). Initial hit-to-lead activities taking advantage of high-throughput parallel synthetic techniques, identified a 1,2-disubstituted benzimidazole 5-carboxylic acid scaffold as the minimum core for biological activity. Potent analogues in this series inhibit the polymerase at low micromolar concentrations and provide an attractive 'drug-like' lead structure for further optimization and the development of potential HCV therapeutics.
- Beaulieu, Pierre L.,Boes, Michael,Bousquet, Yves,Fazal, Gulrez,Gauthier, Jean,Gillard, James,Goulet, Sylvie,LaPlante, Steven,Poupart, Marc-Andre,Lefebvre, Sylvain,McKercher, Ginette,Pellerin, Charles,Austel, Volkhard,Kukolj, George
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p. 119 - 124
(2007/10/03)
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- Synthesis and Chiroptical Properties of Bridged 2,2'-Diaminobiphenyl Derivatives
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The relationship between c.d. spectra and the conformation of chiral 2,2'-diaminobiphenyls was investigated as a function of the torsion angle between the benzene ring planes.The molecular structures of (S)-(+)-4,5,6,7,11,12,13,14-octahydrobenzazocino
- Seno, Kaoru,Hagishita, Sanji,Sato, Tomohiro,Kuriyama, Kaoru
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p. 2012 - 2022
(2007/10/02)
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