- 3,6,13,16-Tetrapropylporphycene: Rational Synthesis, Complexation, and Halogenation
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We have designed and synthesized 3,6,13,16-tetrapropylporphycene for the first time as its alkyl analogue from ethyl 4-propyl-1H-pyrrole-2-carboxylate. The substituent effect was found to be more intense than reported positional isomeric tetrapropylporphycenes. The freebase porphycene exhibited moderate fluorescence and complexation ability with divalent metal ions, including Zn(II), which displayed an enhanced emission quantum yield (~30%). The Pd(II) complex and freebase β-tetrabromoporphycene generated singlet oxygen efficiently (75 and 51%, respectively) and, hence, may find application as potential photosensitizers in photodynamic therapy.
- Nagamaiah, Jodukathula,Dutta, Arnab,Pati, Narendra Nath,Sahoo, Sameeta,Soman, Rahul,Panda, Pradeepta K.
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p. 2721 - 2729
(2022/02/05)
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- Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control
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The Ras/Raf/MEK/ERK signal transduction, an oncogenic pathway implicated in a variety of human cancers, is a key target in anticancer drug design. A novel series of pyrimidylpyrrole ERK inhibitors has been identified. Discovery of a conformational change
- Aronov, Alex M.,Qing, Tang,Martinez-Botella, Gabriel,Bemis, Guy W.,Cao, Jingrong,Chen, Guanjing,Ewing, Nigel P.,Ford, Pamella J.,Germann, Ursula A.,Green, Jeremy,Hale, Michael R.,Jacobs, Marc,Janetka, James W.,Maltais, Francois,Markland, William,Namchuk, Mark N.,Nanthakumar, Suganthini,Poondru, Srinivasu,Straub, Judy,Ter Haar, Ernst,Xiaoling, Xie
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experimental part
p. 6362 - 6368
(2010/03/31)
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- Selective inhibitors of ERK protein kinase and uses thereof
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Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such a
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Page/Page column 22-23
(2008/06/13)
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- PYRROLE DERIVATIVES AS INHIBITORS OF ERK2 AND USES THEREOF
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Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 Are as described in t
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Page/Page column 44
(2010/02/07)
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- Heterocyclic inhibitors of ERK2 and uses thereof
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Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3/sup
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- Synthesis of 2-Alkylputrescines from 3-Alkylpyrroles
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Acylation of 2-(trichloroacetyl)pyrrole gave the 4-acyl derivatives (from 4-formyl to 4-hexanoyl) in good yields.Alkaline treatment gave corresponding 4-acyl-2-pyrrolecarboxylic acids, were decarboxylated to the 3-acylpyrroles by prior conversion to the 3-acyl-2,4,5-triiodopyrroles followed by hydrogenolysis.The 3-acylpyrroles were reduced by treatment with hydrazine in alkaline medium to the 3-alkylpyrroles.The latter were ring-opened by treatment with hydroxylamine in the presence of bicarbonate to give the dioximes of the corresponding 2-alkylsuccinaldehydes, which were then reduced to the 2-alkylpurescines (1,4-diaminobutanes).Ring-opening of 2,3-dimethylpyrrole followed by reduction of the dioxime gave 1,2-dimethylputrescine; the same sequence gave 1,3-dimethylputrescine from 2,4-dimethylpyrrole, while 3,4-dimethylpyrrole did not ring-open and gave the dioxime of 3,4-dimethylmaleimide.
- Garrido, Daniel O. A.,Buldain, Graciela,Ojea, Maria I.,Frydman, Benjamin
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p. 403 - 407
(2007/10/02)
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