- Synthesis and in vitro evaluation of N-Aryl pyrido-quinazolines derivatives as potent epidermal growth factor receptor inhibitors
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A series of pyrido-quinazolines have been synthesised, characterized, and tested for their in vitro epidermal growth factor receptor (EGFR) tyrosine kinase inhibitory activity. The compounds were prepared from Alkylideno/arylideno-bis-ureas. Their final structure of the compounds was elucidated on the basis of spectral studies (IR, 1H NMR, FT-IR, and EI-MS). The cellular EGFR internalization response of selected compounds was evaluated using HeLa cells. Most of the synthesized compounds displayed potent EGFR-TK inhibitory activity and structurally halogenated derivatives had a pronounced effect in inhibiting EGFR internalization.
- Singh, Vinay K.,Sharma, Himanshu,Singh, Sanjay K.,Gangwar, Lakshmi
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p. 119 - 124
(2013/07/26)
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- An investigation leading to preparation of tetrahydro-quinazoline derivatives involving ureidoalkylation and α-amidoalkylation reactions
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Reaction of an aldehyde with excess equivalent of urea in ethanol affords alkylideno/arylideno-bis-ureas 1 which on condensation with p-aminophenol in acidic medium cyclised to 4-aralkyl-6-hydroxy-2-oxo-1,2,3,4- tetrahydroquinazolines 2. Reaction of 2 with arylamidoalcohols in concentrated H2SO4 results in 4-arylkyl-7-arylamido/imidoalkyl-6- hydroxy-2-oxo-1,2,3,4-tetrahydroquinazolines 3, Compounds 3 have been evaluated for their effect on central nervous system (CNS) and cardiovascular system (CVS).
- Pandey,Mukesh,Kumar, Anilesh,Trivedi, Noopur
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experimental part
p. 1910 - 1914
(2009/05/30)
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- Synthesis, antibacterial and antifungal activity of some new pyrido quinazolones
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Alkylideno/arylideno bis ureas 1 synthesized by ureido-alkylation in the presence of alcohols-which on treatment with p-aminobenzoic acid results in 4-aryl-6-carboxylato-1,2,3,4-tetrahydroquinazolines 2. Reaction of 2 with benzoin in presence of polyphosphoric acid yields 4-aryl-8,9-diphenyl-1,4 dihydro-3H, 7-oxo-1,3-diaza anthracene-2,6-dione 3. Condensation of 3 with aromatic primary amine affords N-aryl-8,9-diphenyl (-2-oxopyrido [g]-4-aryl-2-oxo-1,3-dihydro quinazolines 4. The new compound 4 has been screened for their antibacterial and antifungal activities.
- Singh,Pandey
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p. 2745 - 2748
(2007/10/03)
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- Synthesis and pharmacological study of novel pyrido-quinazolone analogues as anti-fungal, antibacterial, and anticancer agents
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A versatile method for novel pyrido-quinazolones was described here and tested for anti-fungal, antibacterial, and anticancerous activities. These synthesized compounds were characterized on the basis of spectroscopic techniques and evaluated for specific radiopharmaceuticals. Preliminary radiolabeling results with 99mTc and biological evaluation studies showed promising results for further evaluation in vivo. The efficiency of labeling was more than 98% and complexes were stable for about 18 h at 25 °C in the presence of serum.
- Tiwari, Anjani K.,Mishra,Bajpai, Aruna,Mishra, Pushpa,Sharma,Pandey,Singh, Vinay Kumar
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p. 4581 - 4585
(2007/10/03)
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- Binding of phenols in the urea-formaldehyde-water system and the role of precondensation stage in the synthesis of polymethyleneurea
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The precondensation stage (keeping of a solution of urea and formaldehyde in a neutral medium) in the synthesis of polymethyleneurea is examined experimentally and by mathematical simulation.
- Maslosh,Zamashchikov,Bezbozhnaya
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p. 1197 - 1200
(2007/10/03)
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