- 17 BETA HSD TYPE 5 INHIBITOR
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To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone; and the present invention has thus been completed.
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Page/Page column 23
(2008/12/08)
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- Synthesis and biological evaluation of bengacarboline derivatives
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Novel derivatives of the marine alkaloid bengacarboline have been synthesized. The seco derivatives 11 and 12 were evaluated for topoisomerase inhibition, DNA damages, cytotoxicity and cell cycle perturbation. The two synthetic analogs are more potent cyt
- Pouilhes, Annie,Kouklovsky, Cyrille,Langlois, Yves,Baltaze, Jean-Pierre,Vispe, Stephane,Annereau, Jean-Philippe,Barret, Jean-Marc,Kruczynski, Anna,Bailly, Christian
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p. 1212 - 1216
(2008/12/21)
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- Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase
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A new series of novel mast cell tryptase inhibitors is reported, which features the use of an indole structure as the hydrophobic substituent on a m-benzylaminepiperidine template. The best members of this series display good in vitro activity and excellent selectivity against other serine proteases.
- Hopkins, Corey R.,Czekaj, Mark,Kaye, Steven S.,Gao, Zhongli,Pribish, James,Pauls, Henry,Liang, Guyan,Sides, Keith,Cramer, Dona,Cairns, Jennifer,Luo, Yongyi,Lim, Heng-Keang,Vaz, Roy,Rebello, Sam,Maignan, Sebastian,Dupuy, Alain,Mathieu, Magali,Levell, Julian
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p. 2734 - 2737
(2007/10/03)
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- First synthesis of marine alkaloid (±)-bengacarboline
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Bengacarboline 1, a marine alkaloid, potent inhibitor of topoisomerase II, has been synthesized in nine steps from indol-3-carboxylic acid and tryptamine.
- Pouilhès, Annie,Langlois, Yves,Chiaroni, Angèle
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p. 1488 - 1490
(2007/10/03)
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- Synthesis of indolo[3,2-c]quinoline and pyrido[3',2':4,5][3,2- c]quinoline derivatives
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Potential antitumoral scaffold indolo[3,2-c]quinoline 5a was obtained by an intramolecular Heck cyclisation from the corresponding 2-iodophenyl-3- indolecarboxamide 4a. The 7-azaindole analogue 5b was prepared by the same approach. Triflate displacement o
- Mouaddib, Abderrahim,Joseph, Beno?t,Hasnaoui, Aissa,Mérour, Jean-Yves
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p. 549 - 556
(2007/10/03)
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