- Synthesis and biological evaluation of new cytotoxic indazolo[4,3-gh] isoquinolinone derivatives
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A series of indazolo[4,3-gh]isoquinolinones derivatives have been synthesized to decrease cardiotoxic side effects in comparison to Mitoxantrone. The antiproliferative effects of different side chains were investigated and tested on at least four different cell lines of cervix, ovarian, CNS, NSCLC (non-small-cell lung cancer) and colon carcinoma. In addition to antiproliferative activities, influence on cell cycle and intercalation behavior have been tested.
- Shahabi, Manochehr,Schirmer, Eva,Shanab, Karem,Leepasert, Theerachart,Ruzicka, Jana,Holzer, Wolfgang,Spreitzer, Helmut,Aicher, Babette,Schmidt, Peter,Blumenstein, Lars,Müller, Gilbert,Günther, Eckhard
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p. 1846 - 1852
(2013/04/10)
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- Antithrombotic amides
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This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermidates thereof.
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- Directed lithiation of unprotected pyridinecarboxylic acids: Syntheses of halo derivatives
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Deprotonation of all isomeric lithium pyridinecarboxylates and subsequent trapping with hexachloroethane or iodine afforded straightforward access to chloro- and iodopyridinecarboxylic acids, respectively. Starting from lithium 5-bromonicotinate, the introduction of an iodine atom at C4 and further halogen migration allowed the potential of this method to be extended to the synthesis of more elaborate derivatives.
- Lazaar, Jalal,Rebstock, Anne-Sophie,Mongin, Florence,Godard, Alain,Trécourt, Fran?ois,Marsais, Francis,Quéguiner, Guy
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p. 6723 - 6728
(2007/10/03)
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- Application of organolithium compounds in organic synthesis. Part 19. Synthetic strategies based on aromatic metallation. A concise regiospecific synthesis of 3-halogenated picolinic and isonicotinic acids
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The synthesis of the halogenated picolin- and isonicotinalides (3) and (4) via metallation (n-BuLi) of the anilides (1) and (2) and then the reaction of the generated bis-lithiated anilides with halogenating agents (CCl3-CCl3, CH2Br-CH2Br, I2) followed by subsequent acidic hydrolysis of (3) and (4), as a way of regiospecific transformation of picoline and isonicotine acids into their C3-halogenated derivatives, is described.
- Epsztajn,Plotka,Grabowska
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p. 1075 - 1086
(2007/10/03)
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- Synthesis of regioisomeric 6,9-(chlorofluoro)-substituted benzo[g]quinoline-5,10-diones, benzo[g]isoquinoline-5,10-diones and 6-chloro-9-fluorobenzo[g]quinoxaline-5,10-dione
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Treatment of difluoro or chloro fluoro-substituted benzyl bromides 5a-c with zinc dust in tetrahydrofuran leads to the corresponding benzylic zinc bromides 6a-c. These organometallics on treatment with chlorosubstituted heterocyclic esters 4A and 4B mediated by nickel catalysis undergo couplings to yield dihalobenzyl substituted heterocyclic esters 7Aa-c and 7Ba-c. Treatment of 4c with 6c under Pd catalysis leads to 7Cc. The acids 8, prepared by hydrolysis of these esters, with treatment of fuming sulfuric acid undergo cyclizations and oxidations to yield the desired regioisomeric dihalo-substituted heterocyclic quinones 2.
- Krapcho, A. Paul,Gallagher, Cynthia E.,Hammach, Abdelhakim,Ellis, Michael,Menta, Ernesto,Oliva, Ambrogio
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