Tumor anti-initiating activity of some novel 3,4-dihydropyrimidinones.
نویسندگان
چکیده
Halting the tumor initiation process by targeting the inhibition of the carcinogens metabolic activators (CYP), the induction of the carcinogen detoxification enzymes (glutathione-S-transferases, GSTs), and the induction of antioxidant activity is an effective strategy. Since several dihydropyrimidine derivatives (Biginelli compounds) are therapeutically active, the present study aimed to synthesize some dihydropyrimidines with multifunctional aromatic substitutions and to investigate their effects as anti-initiating agents. Twelve compounds were synthesized and structurally elucidated. The results revealed that compound 10 was a non-cytotoxic inhibitor of cytochrome P 450 1A (Cyp1A) activity, inducer of GST activity, scavenger of OH and inhibitor of DNA fragmentation. Compounds 1 and 9 were radical scavengers of OH and inhibitors of DNA fragmentation. On the other hand, all compounds were not toxic against different tumor cells, except compounds 2, 4, and 5 possessed non specific cytotoxicity against both liver and colon carcinoma cells, while 7 possessed specific cytotoxicity only against colon carcinoma cells. Compound 1 was a non-cytotoxic inducer of GST activity, scavenger of OH and ROO, and inhibitor of DNA fragmentation. The present study proved that compounds 10 and 1 were active and safe tumor anti-initiating and multi-potent blocking agent.
منابع مشابه
Design, synthesis and pharmacological assay of novel azo derivatives of dihydropyrimidinones
The present work deals with the synthesis of some novel azo derivatives of dihydropyrimidinones. The structures of newly synthesized compounds were established on the basis of their FTIR, 1H NMR, Mass spectrometry and elemental analysis data results. The synthesized agents were assessed for their in vivo anti-inflammatory activity on the Wistar albino rats. The compounds were also screened for ...
متن کاملAn Efficient One-Pot Protocol for the Synthesis of Substituted 3,4-Dihydropyrimidin-2(1H)-ones Using Metallophthalocyanines (MPcs) as Potent Heterogeneous Catalysts: Synthesis, Characterization, Aggregation and Antimicrobial Activity.
In this study, novel phthalonitrile 3 and their corresponding metal-free 4 and metallophthalocyanine derivatives 5-7 bearing 2-isopropenyl-4-methoxy-1-methylbenzene groups were synthesized and characterized. 3,4-Dihydropyrimidinones have been synthesized by a modified Biginelli-type reaction with various metallophthalocyanines 5-7 as catalysts. Compared to the classical Biginielli reaction, the...
متن کاملSynthesis, Antinociceptive, Antiinflammatory and Antiepileptic Evaluation of Some Novel Indeno[1, 2-b] Quinoxalin-11-ylidenamines
A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, ...
متن کاملBrønsted Acidic Ionic Liquid: An Efficient and Reusable Catalyst for the Multi-Component Synthesis of Dihydropyrimidinones under Solvent-Free Conditions
An efficient and convenient procedure for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones and thiones by condensation of 1,3-dicarbonyl compounds, Aromatic and aliphatic aldehydes, and urea or thiourea in the presence of catalytic amount of Brønsted acidic ionic liquid 3-methyl-1-sulfonic acid imidazolium chloride {[Msim]Cl} under thermal solvent-free conditions reacted easily to afford the co...
متن کاملSynthesis of 4-aryl substituted 3,4-dihydropyrimidinones using silica-chloride under solvent free conditions.
This paper describes an improved procedure for the efficient and facile synthesis of 4-aryl substituted 3, 4-dihydropyrimidinones under mild reaction conditions with excellent yields using inexpensive silica chloride under solvent free conditions.
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Pharmacological reports : PR
دوره 61 6 شماره
صفحات -
تاریخ انتشار 2009