- Asymmetrical 2,6-bis(benzylidene)cyclohexanones: Synthesis, cytotoxic activity and QSAR study
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In order to develop novel anti-cancer agents, a series of asymmetrical 2,6-bis (benzylidene)cyclohexanone derivatives containing nitrobenzylidene moiety were synthesized and their cytotoxic activity were determined in vitro against MDA-MB 231, MCF-7 and SK-N-MC cell lines using MTT assay. Among the tested compounds, the highest activity against MDA-MB 231 cells was achieved by 2-(3-bromo-5-methoxy-4-propoxybenzylidene)-6-(2-nitrobenzylidene)cyclohexanone (compound 5d). Whereas, compound 5j (the 3-nitro analog of compound 5d) was the most potent compound against MCF-7 and SK-N-MC cell lines. The results indicated that the cytotoxic activity profile against different tumor cells can be optimized by desired 4-alkoxy-3-bromo-5-methoxybenzylidene scaffold.
- Nakhjiri, Maryam,Safavi, Maliheh,Alipour, Eskandar,Emami, Saeed,Atash, Amir Farzin,Jafari-Zavareh, Mona,Ardestani, Sussan K.,Khoshneviszadeh, Mehdi,Foroumadi, Alireza,Shafiee, Abbas
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experimental part
p. 113 - 123
(2012/07/03)
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- SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS
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The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds
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Page/Page column 191
(2011/12/14)
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- Sulfur Analogues of Psychotomimetic Agents. 3. Ethyl Homologues of Mescaline and Their Monothio Analogues
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All possible monothio analogues of the mono-, di-, and triethoxy homologues of mescaline have been synthesized and pharmacologically evaluated in man.Modifications at the ring position para to the ethylamine chain, either with a sulfur atom, a longer alkyl chain, or both, lead to compounds of high central nervous system activity.The 4-n-propoxy and 4-n-butoxy homologues and their corresponding 4-thio analogues were also synthesized and pharmacologically evaluated.The propyl homologues retain high potency, but a butyl group (either with or without a sulfur atom) leads to a decrease in activity.The m-ethyl or m-thio analogues retain some central action but the diethoxy and especially the triethoxy homologues are relatively inactive as psychotomimetic drugs.
- Jacob, Peyton,Shulgin, Alexander T.
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p. 881 - 888
(2007/10/02)
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