An overview on synthetic and pharmaceutical prospective of pyrido[2,3‐<i>d</i>]pyrimidines scaffold

Yadav, Pratibha; Shah, Kamal

doi:10.1111/cbdd.13800

Cited by 33 publications

(14 citation statements)

References 76 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Pyridopyrimidines and other N-heterocycles are of great interest due to their biological potential. The pyridopyrimidine moiety is present in relevant drugs and, in recent years, it has been studied in the development of new therapies, as evidenced by numerous publications, studies and clinical trials [1][2][3]. The various pyridopyrimidines are used on several therapeutic targets.…”

Section: Introduction: Pyridopyrimidines and Their Scaffoldmentioning

confidence: 99%

Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

2022

View full text Add to dashboard Cite

The objective of this review is to list the structures composed of a pyridopyrimidine moiety which have shown a therapeutic interest or have already been approved for use as therapeutics. We consider all the synthetic protocols to prepare these pyridopyrimidine derivatives. The review is organized into four sections, successively pyrido[2,3-d]pyrimidines, pyrido[3,4-d]pyrimidines, pyrido[4,3-d]pyrimidines and pyrido[3,2-d]pyrimidines. For each compound we present the biological activity and the synthetic route reported. To produce this manuscript, the bibliographic research was done using Reaxys and Scifinder for each kind of pyridopyrimidine.

show abstract

Section: Introduction: Pyridopyrimidines and Their Scaffoldmentioning

confidence: 99%

Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

2022

View full text Add to dashboard Cite

show abstract

“…On the other hand, the traditional synthetic tactics had a good impact on pyridopyrimidine derivatives for new name reactions such as tandem aza‐witing reaction, annulations, and Biginelli‐type reactions. Recently, it has been found that a highly efficient regioselective/Staudinger/intramolecular cyclization of alkyne reaction has been used for the synthesis of substituted pyridopyrimidine derivatives (Yadav & Shah, 2021).…”

Section: Introductionmentioning

confidence: 99%

Chemistry and biological evaluation of pyrido[4,3‐d]pyrimidines: A review

Yadav

Shah

2022

Chem Biol Drug Des

Self Cite

View full text Add to dashboard Cite

The aim of this review is to update the knowledge of different multi‐component reactions that lead to synthesizing of pyrido[4,3‐d]pyrimidines. In this study, the multiple synthetic pathways that are discussed in the synthesis of pyrido[4,3‐d]pyrimidines lead are highlighted. Thus, the developed compounds have been derived from pyridine and pyrimidines fusion or from possible approaches of multistep synthesis reaction versatility. Apart from the synthetic schemes, their biological applications are also comprehended. This review discusses that the pyrido[4,3‐d]pyrimidines have been developed by using new strategies and may be useful to future researchers.

show abstract

“…The pyridopyrimidine skeletons appear in the literature including pyrido[2,3- d ]pyrimidine, pyrido[3,2- d ]pyrimidine, pyrido[3,4- d ]pyrimidine, and pyrido[4,3- d ]pyrimidine (Figure ). Pyrido[2,3- d ]pyrimidine is commonly used in the kinase inhibitors of AKT, ARK5, CDK4, CDK6, c-Met, c-Src, DYRK1A, DYRK1B, eEF2K, EGFR, EGFR T790M , ERK1/2, FGFR1, FGFR3, MEK, PDGFR, PI3K/mTOR, and RAF . Other types of pyridopyrimidines are rarely used in the kinase inhibitor design.…”

Section: Introductionmentioning

confidence: 99%

“…Pyrido[2, 3-d]pyrimidine is commonly used in the kinase inhibitors of AKT, ARK5, CDK4, CDK6, c-Met, c-Src, DYRK1A, DYRK1B, eEF2K, EGFR, EGFR T790M , ERK1/2, FGFR1, FGFR3, MEK, PDGFR, PI3K/mTOR, and RAF. 26 Other types of pyridopyrimidines are rarely used in the kinase inhibitor design. Pyrido [3,4-d]pyrimidine appears in the inhibitors of EGFR and monopolar spindle kinase 1 (MPS1).…”

Section: ■ Introductionmentioning

confidence: 99%

Optimization of 4,6-Disubstituted Pyrido[3,2-d]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth

et al. 2021

View full text Add to dashboard Cite

Mitogen-activated protein kinase-interacting kinases (MNKs) and provirus integration in maloney murine leukemia virus kinases (PIMs) are downstream enzymes of cell proliferation signaling pathways associated with the resistance of tyrosine kinase inhibitors. MNKs and PIMs have complementary effects to regulate cap-dependent translation of oncoproteins. Dual inhibitors of MNKs and PIMs have not been developed. We developed a novel 4,6-disubstituted pyrido[3,2-d]pyrimidine compound 21o with selective inhibition of MNKs and PIMs. The IC50’s of 21o to inhibit MNK1 and MNK2 are 1 and 7 nM and those to inhibit PIM1, PIM2, and PIM3 are 43, 232, and 774 nM, respectively. 21o inhibits the growth of myeloid leukemia K562 and MOLM-13 cells with GI50’s of 2.1 and 1.2 μM, respectively. 21o decreases the levels of p-eIF4E and p-4EBP1, the downstream products of MNKs and PIMs, as well as cap-dependent proteins c-myc, cyclin D1, and Mcl-1. 21o inhibits the growth of MOLM-13 cell xenografts without causing evident toxicity. 21o represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

show abstract

An overview on synthetic and pharmaceutical prospective of pyrido[2,3‐d]pyrimidines scaffold

Cited by 33 publications

References 76 publications

Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

Review on the Synthesis and Therapeutic Potential of Pyrido[2,3-d], [3,2-d], [3,4-d] and [4,3-d]pyrimidine Derivatives

Chemistry and biological evaluation of pyrido[4,3‐d]pyrimidines: A review

Optimization of 4,6-Disubstituted Pyrido[3,2-d]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth

Contact Info

Product

Resources

About