- β-Lactam analogues of combretastatin A-4 prevent metabolic inactivation by glucuronidation in chemoresistant HT-29 colon cancer cells
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Glucuronidation by uridine 5-diphosphoglucuronosyl transferase enzymes (UGTs) is a cause of intrinsic drug resistance in cancer cells. Glucuronidation of combretastatin A-4 (CA-4) was previously identified as a mechanism of resistance in hepatocellular ca
- Malebari, Azizah M.,Greene, Lisa M.,Nathwani, Seema M.,Fayne, Darren,O'Boyle, Niamh M.,Wang, Shu,Twamley, Brendan,Zisterer, Daniela M.,Meegan, Mary J.
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p. 261 - 285
(2017/03/09)
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- COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY
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Compounds of formula (I): wherein X, L1, R1, L2, R2, R3, and R4 are as defined herein, are useful in the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.
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Page/Page column 53
(2010/12/29)
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- Synthesis and serotonin transporter activity of sulphur-substituted α-alkyl phenethylamines as a new class of anticancer agents
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The discovery that some serotonin reuptake transporter (SERT) ligands have the potential to act as pro-apoptotic agents in the treatment of cancer adds greatly to their diverse pharmacological application. 4-Methylthioamphetamine (MTA) is a selective ligand for SERT over other monoamine transporters. In this study, a novel library of structurally diverse 4-MTA analogues were synthesised with or without N-alkyl and/or C-α methyl or ethyl groups so that their potential SERT-dependent antiproliferative activity could be assessed. Many of the compounds displayed SERT-binding activity as well as cytotoxic activity. While there was no direct correlation between these two effects, a number of derivatives displayed anti-tumour effects in lymphoma, leukaemia and breast cancer cell lines, showing further potential to be developed as possible chemotherapeutic agents.
- Cloonan, Suzanne M.,Keating, John J.,Butler, Stephen G.,Knox, Andrew J.S.,Jorgensen, Anne M.,Peters, Guenther H.,Rai, Dilip,Corrigan, Desmond,Lloyd, David G.,Williams, D. Clive,Meegan, Mary J.
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scheme or table
p. 4862 - 4888
(2010/01/16)
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- NOVEL IMIDAZOLES WITH ANTI-INFLAMMATORY ACTIVITY
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Compounds of formula I wherein: one of X or Y represents N and the other represents C; R1 represents hydrogen, methyl, halogen, cyano, nitro, -CHO, -COCH3 or -COOR4; R2 represents optionally-substituted aryl or heteroaryl; R3 represents C1-8 alkyl, C1-8 haloalkyl or -NR4R6; R4 represents hydrogen, C1-8 alkyl or arylC0-8 alkyl; R6 represents hydrogen, C1-8 alkyl, arylC1-8 alkyl, -COR8 or -COOR8; R8 represents C1-8 alkyl or C1-8 haloalkyl; aryl in the above definitions represents phenyl or naphthyl; and heteroaryl in the above definitions represents pyridine, pyrazine, pyrimidine or pyridazine, which can be optionally fused to a benzene ring. These compounds are useful as cyclooxygenase-2 inhibitors.
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- Reaction of Styrene 3,4-Oxide with Ethanediol and Dehydration to Ethylthiostyrenes
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Styrene 3,4-oxide reacts with the nucleophile ethanediol, and the product is dehydrated to give three isomeric ethylthiostyrenes via the corresponding ethylthiovinylcyclohexadienols without formation of thiiranium ions as intermediates.
- Watabe, Tadashi,Hiratsuka, Akira,Sone, Tomomichi,Ishihama, Tetsuya
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p. 585 - 586
(2007/10/02)
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