Synthesis of a new series of pyrimidine derivatives: exploration of anti-proliferative activity on EAT cells and molecular docking

Senthilkumar, N.; Ravichandran, Y. Dominic; Kumar, K. M.; Ramaiah, Sudha

doi:10.1007/s11164-015-2086-2

Cited by 3 publications

(3 citation statements)

References 42 publications

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“…Pyrimidine ring based anti-cancer drug methotrexate (MTX) was used as a standard for the new series of pyrimidine derivatives for AD and anti-cancer activity [ 62 ].…”

Section: Introductionmentioning

confidence: 99%

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Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

Singh

Dhanawat²,

Gupta

et al. 2020

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: Alzheimer’s disease (AD) is a multifarious and developing neurodegenerative disorder. The treatment of AD is still a challenge and availability of drug therapy on the basis of symptoms is not up to the mark. In the context of the existence, which is getting worse for the human brain, is necessary to taken care of the all critical measures. The disease causes due to multidirectional pathology of the body, which demands the multi-target-directed ligand (MTDL) approach and provides a hope for the new drugs for AD, which is summarized herein with the pyrimidine based natural product inspired molecule as a lead. The review is sufficient to provide a list of chemical ingredients of the plant to cure the AD and screened them against the various potential targets of the AD. The synthesis of a highly functionalized scaffold in one step in one pot without isolating the intermediate is a challenging task, but in a few examples, we have highlighted the importance of this kind of reaction, generally known as multi-component reaction. The multi-component is widely accepted technique by the drug discovery people due to its high atom economy and it reduces multi-step process to a one-step process, so, the compounds library can be made in minimum time and cost. This review has highlighted the importance of multicomponent reactions by giving the example of active scaffolds of pyrimidine/fused pyrimidines. This would bring to the importance of the fast as well as a smart synthesis of the bio-relevant molecules.

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“…Pyrimidine ring based anti-cancer drug methotrexate (MTX) was used as a standard for the new series of pyrimidine derivatives for AD and anti-cancer activity [ 62 ].…”

Section: Introductionmentioning

confidence: 99%

“…The pyrimidine scaffold ( 4 ) was further functionalised through three steps to get the final pyrimidine derivatives ( 5 ) (Fig. 8 ) [ 62 ].…”

Section: Introductionmentioning

confidence: 99%

Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

Singh

Dhanawat²,

Gupta

et al. 2020

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“…Indole derivatives have been reported to possess a variety of physiological and pharmacological activities like antibacterial [22], antifungal [23], antioxidant [24], anticancer [25], analgesic [26], antiasthma mine [27] and antiviral [28] and to be effective in treatment of sexual dysfunction [29]. Similarly, a in vitro Cytotoxic Evaluation of Some New Synthesized Pyridazine Derivatives large number of pyrimidine derivatives are reported to exhibit antimicrobial [30], anticancer [31], antiangiogenic [32], antitumor [33], antiproliferative [34], antihistaminic [35], antiviral and antibacterial activities [36]. This prompted the authors to synthesize a new pyrimidine derivative through the reaction of compound 17 with malonic acid to give the corresponding thioxodihydropyrimidinedione (19).…”

Section: Introductionmentioning

confidence: 99%

in vitro Cytotoxic Evaluation of Some New Synthesized Pyridazine Derivatives

Nabil

Al-Dossary

2019

Asian J. Chem.

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A series of novel pyridazine, pyrazoles, pyrimidines derivatives have been synthesized through the reaction of chloropyridazine (1) with p-phenylenediamine to give compound 2. Diazotization of compound 2 followed by coupling with active methylene compounds namely acetylacetone, ethylcyanoacetate and/or ethylacetoacetate afforded novel hydrazons derivatives (4-6). The resulting hydrazons can have been cyclized using hydrazine hydrate and guanidine gave the corresponding pyrazoles (7-9) and pyimidine (10) derivatives. Reaction of compound 2 with acrylonitrile, aromatic aldehyde, p-chloroacetophenone and phenyl isothiocyanate gave compounds 11, 12a, 12b, 13 and 17, respectively. The latter compounds have been used in synthesis of some heterocyclic compounds. The cytotoxic activity of the most active compounds was assessed in vitro against breast carcinoma cell line (MCF-7), human liver cancer cell line (HEPG2), human colon cancer cell line (HCT). Compounds 4, 8 showed best activity against MCF-7 cell line, compounds 5, 13a showed best activity against HePG2 cell line and compound 10 showed best activity against HCT cell line.

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TMU-16-NH ₂ : A Metal–Organic Framework as an Efficient, Green, and Heterogeneous Catalyst for the Michael Addition Annulations for the Synthesis of a New Series of 2,4-Diphenylpyrido[4,3-d]Pyrimidines

Nikseresht,

Shokri,

Mohammadi

et al. 2023

Polycyclic Aromatic Compounds

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Synthesis of a new series of pyrimidine derivatives: exploration of anti-proliferative activity on EAT cells and molecular docking

Cited by 3 publications

References 42 publications

Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

in vitro Cytotoxic Evaluation of Some New Synthesized Pyridazine Derivatives

TMU-16-NH ₂ : A Metal–Organic Framework as an Efficient, Green, and Heterogeneous Catalyst for the Michael Addition Annulations for the Synthesis of a New Series of 2,4-Diphenylpyrido[4,3-d]Pyrimidines

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Synthesis of a new series of pyrimidine derivatives: exploration of anti-proliferative activity on EAT cells and molecular docking

Cited by 3 publications

References 42 publications

Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease

in vitro Cytotoxic Evaluation of Some New Synthesized Pyridazine Derivatives

TMU-16-NH 2 : A Metal–Organic Framework as an Efficient, Green, and Heterogeneous Catalyst for the Michael Addition Annulations for the Synthesis of a New Series of 2,4-Diphenylpyrido[4,3-d]Pyrimidines

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TMU-16-NH ₂ : A Metal–Organic Framework as an Efficient, Green, and Heterogeneous Catalyst for the Michael Addition Annulations for the Synthesis of a New Series of 2,4-Diphenylpyrido[4,3-d]Pyrimidines