Synthesis, cytotoxicity and hDHFR inhibition studies of 2H-pyrido[1,2-a]pyrimidin-2-ones

Rapolu, Sreevani; Manjula, A.; Ganji, Roopa Jones; Saddanapu, Venkateshwarlu; Kishor, Chandan; Bommena, Vittal Rao; Addlagatta, A.

doi:10.1039/c3md00013c

Cited by 19 publications

(17 citation statements)

References 25 publications

(18 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Rapolu et al studied the DHFR inhibitory effect and the anticancer properties of novel substituted 2 H -pyrido[1,2- a ]pyrimidin-2-ones. Among these, compound 17 (Figure 8) emerged as the most potent inhibitor, displaying submicromolar inhibition against DHFR (IC 50 3.1μM) and a good cytotoxicity (IC 50 lower than 10 μM) against MCF-7 and SK-n-SK [51]. The series of 6-substituted pyrimidine synthesized by Gangjeeet al should also be mentioned, since compound 18 not closely related to the other DHFR drugs appears to be a promising DHFR inhibitors candidate [52].…”

Section: Inhibitors Of Human Dhfr Under Preclinical Investigationmentioning

confidence: 99%

DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents

et al. 2019

View full text Add to dashboard Cite

Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, in order to thoroughly delineate the current landscape for medicinal chemists interested in furthering this study in the anticancer field.

show abstract

Section: Inhibitors Of Human Dhfr Under Preclinical Investigationmentioning

confidence: 99%

DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents

et al. 2019

View full text Add to dashboard Cite

show abstract

“…Pyridopyrimidine derivatives are also known as antidepressant, 18 gastrointestinal protective, 19 neurotropic and stressprotecting, 20 and anticancer agents. 21 pyrido[1,2-a]pyrimidine constitutes the core structure of some marketed drugs, including the antiasthmatic agent pemirolast, 22 the tranquilizer pirenperone, 23 and the antiallergic agent ramastine 24 (Fig.…”

Section: Introductionmentioning

confidence: 99%

An efficient synthesis of new imidazo[1,2-a]pyridine-6-carbohydrazide and pyrido[1,2-a]pyrimidine-7-carbohydrazide derivatives via a five-component cascade reaction

Hosseini

Bayat

2019

RSC Adv.

View full text Add to dashboard Cite

show abstract

“…Among them, pyrido[1,2‐a]pyrimidines exist in the structure of several prescribed drugs such as the tranquilizer, pirenperone, antiasthmatic agent, pemirolast, antiallergic agent, barmastine, and antiulcerativeagent . They are also renowned for their antidepressant, stress‐protecting, gastrointestinal protective, neurotropic, and anticancer properties . They also exhibit promising antiviral, (anti‐HIV), antibacterial and antinociceptive activities (Figure ).…”

Section: Introductionmentioning

confidence: 99%

Metal‐Free Assemblage of Four C−N and Two C−C Bonds via a Cascade Five Component Diastereoselective Synthesis of Pyrido[1,2‐a]Pyrimidines

2018

View full text Add to dashboard Cite

An efficient heteroannulation synthesis of N‐fused, pyrido[1,2‐a]pyrimidines was successfully achieved via a sequential, one‐pot five‐component reaction, involving primary amines, diketene (DK), differently substituted aromatic aldehydes, nitro ketene dithioacetal and propanediamine in ethanol at 70 °C. This new protocol constructs two rings through the formation of four C–N and two C–C bonds via a one pot sequential reaction involving ring‐opening/ Knoevenagel condensation, /nucleophilic substitution (SN)/ Michael addition followed by imine−enamine tautomerization and final N‐heterocyclization. The method is particularly attractive due to the advantages such as: atom economy, optimum convergence, commercially available or readily accessible starting materials, high bond‐forming efficiency, free metal‐catalyst and mild reaction conditions. The products were isolated by just decantation of the solvent and purification without using column chromatography method.

show abstract

Synthesis, cytotoxicity and hDHFR inhibition studies of 2H-pyrido[1,2-a]pyrimidin-2-ones

Cited by 19 publications

References 25 publications

DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents

DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents

An efficient synthesis of new imidazo[1,2-a]pyridine-6-carbohydrazide and pyrido[1,2-a]pyrimidine-7-carbohydrazide derivatives via a five-component cascade reaction

Metal‐Free Assemblage of Four C−N and Two C−C Bonds via a Cascade Five Component Diastereoselective Synthesis of Pyrido[1,2‐a]Pyrimidines

Contact Info

Product

Resources

About