- Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents
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A series of 1-phenyl-[1,2,4]triazolo[4,3-a]quinazolin-5-ones designed as conformationally restricted CA-4 analogues, were tested for their tubulin polymerization and growth inhibitory activities. The 3-hydroxy-4-methoxy derivatives 11d and 12d are potent inhibitors of tubulin assembly but only the N-methylated amid counterpart 12d possesses potent anticancer activity in a large panel of cancer cell lines. Upon treatment with compound 12d, remarkable cell shape changes as cell migration and tube formation were elicited in HUVECs, consistent with vasculature damaging activity.
- Driowya, Mohsine,Leclercq, Julien,Verones, Valerie,Barczyk, Amélie,Lecoeur, Marie,Renault, Nicolas,Flouquet, Nathalie,Ghinet, Alina,Berthelot, Pascal,Lebegue, Nicolas
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p. 393 - 405
(2016/04/06)
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- Synthesis of novel quinazoline-4-one derivatives and their acyclonucleoside analogs
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A number of quinazolin-4-one derivatives were synthesized. Reaction of the 2-hydrazonoquinazoline-4-one derivatives with aldoses afforded the corresponding sugar hydrazones which on treatment with ferric chloride to afford the corresponding acyclic nucleoside analogues.
- Zahran, Magdy A.-H.,Ali, Omar M.,Zeid, Ibrahim F.,Rageb, Elham
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experimental part
p. 2121 - 2124
(2012/08/28)
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- New pyrazoline bearing 4(3H)-quinazolinone inhibitors of monoamine oxidase: Synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity
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A new series of pyrazoline derivatives were prepared starting from a quinazolinone ring and evaluated for antidepressant, anxiogenic and MAO-A and -B inhibitory activities by in vivo and in vitro tests, respectively. Most of the synthesized compounds show
- Goekhan-Kelekci, Nesrin,Koyunoglu, Semra,Yabanoglu, Samiye,Yelekci, Kemal,Oezgen, Oezen,Ucar, Guelberk,Erol, Kevser,Kendi, Engin,Yesilada, Akguel
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scheme or table
p. 675 - 689
(2009/06/28)
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- Synthesis of new 4(3H)-quinazolinone derivatives using 5(4H)-oxazolones
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New derivatives of 5(4H)-quinazolinone containing 2-imidazolin-5-one rings have been prepared from 5(4H)-oxazolone derivatives.
- Hamidian, Hooshang,Tikdari, Ahmad Momeni,Khabazzadeh, Hojatollah
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p. 377 - 382
(2007/10/03)
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- Regioselectivity of electrophilic attack on 4-methyl-1-thioxo-1,2,4,5- tetrahydro[1,2,4]triazolo[4,3-a]quinazolin-5-one. Part 1: Reactions at the sulfur atom
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The regioselectivity of the model compound 4-methyl-1-thioxo-1,2,4,5- tetrahydro[1,2,4]triazolo[4,3-a]quinazolin-5-one (3) towards different electrophiles was studied. Compound 3 reacts with alkyl and aryl halides to give the corresponding S-substituted derivatives. The reaction of the model thioamide with acyl halides proceeds by the formation of kinetically controlled S-acyl derivatives followed by a transacylation reaction to give the N 2-acyl derivatives as thermodynamically controlled products. Theoretical DFT computational studies supported the explanation of these results. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR, and mass spectroscopy.
- Fathalla, Walid,Cajan, Michal,Pazdera, Pavel
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p. 557 - 573
(2007/10/03)
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- Pesticidal dihydrotetrazolo [1,5-a] quinazoline compound and processes and compositions for using the same
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A dihydrotetrazolo[1,5-a]quinazoline compound which in free base form has the formula: STR1 wherein R3 is hydrogen, hydroxy or dialkylamino of from 1 to 4 carbon atoms; R2 is dialkylamino when R3 is dialkylamino and R2 is hydrogen when R3 is hydrogen or hydroxy; and R is a lower alkyl of from 1 to 4 carbon atoms. Pesticidal compositions containing such compound and priocesses for using the same to combat pests, especially fungi, are also disclosed.
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