Synthesis of Some Novel Pyrido[2,3‐d]pyrimidine and Pyrido[3,2‐e][1,3,4]triazolo and Tetrazolo[1,5‐c]pyrimidine Derivatives as Potential Antimicrobial and Anticancer Agents

AbedelRehim, Elsayed Mohmoud; Abdel-Latif, Mohamed S.

doi:10.1002/jhet.3058

Cited by 16 publications

(8 citation statements)

References 15 publications

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“…In a parallel study HepG-2 and HCT-116 cancer cell lines were screened by novel pyrido[2,3-d]pyrimidine derivatives and 80(a-d) were found to be most active (Fig. 26) [83]. Pyrido [2,3- 3-a]pyrimidine derivatives and pyrido [2,3-d]pyrimidines were evaluated against two cancer cell lines, namely PC-3 and A-549.…”

Section: Pyrido[23-d]pyrimidine Derivativesmentioning

confidence: 99%

Pyrimidine: a review on anticancer activity with key emphasis on SAR

2021

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Background Cancer is a global health challenge, it impacts the quality of life and its treatment is associated with several side effects. Resistance of the cancer cells to the existing drugs has led to search for novel anticancer agents. Pyrimidine, a privileged scaffold, is part of living organisms and plays vital role in various biological procedures as well as in cancer pathogenesis. Due to resemblance in structure with the nucleotide base pair of DNA and RNA, it is recognized as valuable compound in the treatment of cancer. Main text Many novel pyrimidine derivatives have been designed and developed for their anticancer activity in the last few years. The present review aims to focus on the structure activity relationship (SAR) of pyrimidine derivatives as anticancer agent from the last decade. Conclusion This review intends to assist in the development of more potent and efficacious anticancer drugs with pyrimidine scaffold. Graphical abstract

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Section: Pyrido[23-d]pyrimidine Derivativesmentioning

confidence: 99%

Pyrimidine: a review on anticancer activity with key emphasis on SAR

2021

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“…Continuing our interest in preparing of new heterocyclic compounds and examining their various biological activities [ 1 – 6 ], this work was designed to prepare new derivatives of condensed and non-condensed five-membered rings with pyrimidine. Pyrimidine derivatives have aroused the interest of researchers in recent years, as they have demonstrated a wide variety of biological activities such as antibacterial [ 6 ], antiallergic, antihypertensive [ 7 ] and antitumor activity [ 5 , 8 ], along with their cardiopulmonary and bronchodilating effect [ 9 ]. It has been observed that the substitution of the benzene ring in pyrimidine derivatives with heterocyclic moieties such as pyrrole and thiophene shows some biological activities such as anti-proliferative and anti-inflammatory activities [ 10 – 12 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, screening as potential antitumor of new poly heterocyclic compounds based on pyrimidine-2-thiones

Abdelrehim

Soliman

2022

BMC Chemistry

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Background Continuing our interest in preparing of new heterocyclic compounds and examining their various biological activities, this work was designed to prepare new condensed and non-condensed heterocyclic compounds 9a-c, 10a-c, 11a-c, 13a-c and 14a-c were synthesized starting with pyrimidine-2-thiones 4a-c. Results Thiazolo[3,2-a]pyrimidines 9a-c were synthesized by S-alkylation of pyrimidine-2-thiones,4a-c, internal cyclization in alkaline medium with ammonia, condensation with benzaldehyde and finally reaction with hydroxylamine hydrochloride.[1,2,4]thiadiazolo[4,5-a]pyrimidines 11a-c were formed by heating of the 4a-c with benzoylcholride to afford 10a-c followed by reaction with sodium hypochlorite, ammonia and sodium hydroxide. Cyclocondensation of 4a-c with ethyl acetoacetate or formic acid yielded pyrazol-3-ones 13a-c or [1,2,4] triazolo[4,3-a]pyrimidines 14a-c, respectively Elements analysis, IR, 1H-NMR, 13C-NMR and mass spectra were used to validate the structures of newly synthesized heterocycles. Screening of the selected compounds 4a, 6a, 7a, 9a, 10a, 13a and 14a against colon carcinoma cell lines (HCT-116) and hepatocellular carcinoma cell lines (HepG-2). Conclusions Elements analysis, IR, 1H-NMR, 13C-NMR and mass spectra were used to validate the structures of newly synthesized heterocycles. Screening of the selected compounds 4a, 6a, 7a, 9a, 10a, 13a and 14a against colon carcinoma cell lines (HCT-116) and hepatocellular carcinoma cell lines (HepG-2) showed that compound 10a exhibited the most cytotoxic, while compounds 4a, 6a and 14a exhibited considerable cytotoxic activity.

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“…In general, pyrido [2,3-d]pyrimidines derivatives are extremely important for their biological activities. For example, some are antitumor [51,52], antibacterial [52], anticonvulsant [53], antipyretic [54], analgesic, and CNS depressant activity [55]. Thus, heating compound 1a with 2-(4-methoxybenzylidene) malononitrile in ethanol under refluxing in the presence of a catalytic amount of ammonium acetate leads to the formation of 7-aminopyrido [2, 3-d] pyrimidine carbonitrile derivative 9.…”

Section: Chemistrymentioning

confidence: 99%

Synthesis and characterization of the novel pyrimidine’s derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity

et al. 2021

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Herein, the biological activities including antibacterial, antifungal, and in-vitro cytotoxicity for some novel substituted pyrazolo [3,4-d]pyrimidinone, benzylidene dihydropyrimidine, pyrano [2,3-d]pyrimidine, hexahydropyrimido[4, 5-d]pyrimidinone, tetrahydropyrido[2,3-d]pyrimidine-6-carbonitrile, and pyrido[2, 3-d:6,5-d'] dipyrimidinone derivatives were investigated. The synthesized novel compounds were achieved through the incorporation of the active moieties such as halo compound, pyrazolo, pyrano, pyrimido, pyrido-derivatives with active methylene group in thiobarbituric acid derivatives at C-5. Structures of all synthesized compounds were characterized by spectral techniques including IR, 1 H-NMR, MS, and 13 C-NMR. All synthesized compounds were screened for their antibacterial and antifungal activity, while the most promising compounds were selected to investigate their in-vitro cytotoxic efficacy against normal Vero cells and cancerous Caco-2 cells. Data showed that the biological activities were concentration-dependent. All novel pyrimidine derivatives exhibited broad-spectrum antimicrobial activity with a varied zone of inhibition ranging between 11.3 ± 0.6 and 25.3 ± 0.6 mm. The MIC values are different according to a pathogenic organism (ranging between 3.91 and 500 µg mL −1 ), whereas the MBC/ MFC were 2 × to 4 × MIC value. Data of in-vitro cytotoxicity confirm the efficiency of selected novel pyrimidine derivatives to target Caco-2 cancerous cells at low concentrations more Vero normal cells. Four selected compounds 4, 7b, 10, and

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Synthesis of Some Novel Pyrido[2,3‐d]pyrimidine and Pyrido[3,2‐e][1,3,4]triazolo and Tetrazolo[1,5‐c]pyrimidine Derivatives as Potential Antimicrobial and Anticancer Agents

Cited by 16 publications

References 15 publications

Pyrimidine: a review on anticancer activity with key emphasis on SAR

Pyrimidine: a review on anticancer activity with key emphasis on SAR

Synthesis, screening as potential antitumor of new poly heterocyclic compounds based on pyrimidine-2-thiones

Synthesis and characterization of the novel pyrimidine’s derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity

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