Implication of Quinazoline-4(3H)-ones in Medicinal Chemistry: A Brief Review

Tiwary, Bipransh Kumar; Pradhan, Kiran; Nanda, Ashis Kumar; Chakraborty, Ranadhir

doi:10.4172/2572-0406.1000104

Cited by 23 publications

(19 citation statements)

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“…Each of these structures has found several uses depending on molecular structure. There are many examples for quinoline alkaloids such as mefloquine as antimalarial agent, fluoroquinolone antibiotics and topotecan as anticancer drug, just to name a few (Collin and Höke, 2000;Tiwary et al, 2015). The latter two work as inhibitors of different DNA topoisomerases (Lemmer and Brune, 2004).…”

Section: Phytochemicalsmentioning

confidence: 99%

Phytochemicals: Potential Lead Molecules for MDR Reversal

2020

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Multidrug resistance (MDR) is one of the main impediments in the treatment of cancers. MDR cancer cells are resistant to multiple anticancer drugs. One of the major mechanisms of MDR is the efflux of anticancer drugs by ABC transporters. Increased activity and overexpression of these transporters are important causes of drug efflux and, therefore, resistance to cancer chemotherapy. Overcoming MDR is a fundamental prerequisite for developing an efficient treatment of cancer. To date, various types of ABC transporter inhibitors have been employed but no effective anticancer drug is available at present, which can completely overcome MDR. Phytochemicals can reverse MDR in cancer cells via affecting the expression or activity of ABC transporters, and also through exerting synergistic interactions with anticancer drugs by addressing additional molecular targets. We have listed numerous phytochemicals which can affect the expression and activity of ABC transporters in MDR cancer cell lines. Phytochemicals in the groups of flavonoids, alkaloids, terpenes, carotenoids, stilbenoids, lignans, polyketides, and curcuminoids have been examined for MDR-reversing activity. The use of MDR-reversing phytochemicals with low toxicity to human in combination with effective anticancer agents may result in successful treatment of chemotherapy-resistant cancer. In this review, we summarize and discuss published evidence for natural products with MDR modulation abilities.

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Section: Phytochemicalsmentioning

confidence: 99%

Phytochemicals: Potential Lead Molecules for MDR Reversal

2020

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“…Indeed, they possess a wide range of biological activities, such as antimalarial, anticancer, antimicrobial, sedative, anesthetic, anti-inflammatory, Quinazolines and quinazolinones constitute a class of biologically active nitrogen heterocyclic compounds with high therapeutic potential. Indeed, they possess a wide range of biological activities, such as antimalarial, anticancer, antimicrobial, sedative, anesthetic, anti-inflammatory, antileishmanial, antidepressant, and many others [107,108]. Several drugs contain a quinazoline or quinazolinone ring, such as dacomitinib, alfusozine, bunazosin, Gefitinib, proquazone, letermovir, and afatinib [107].…”

Section: Ultrasound-assisted Synthesis Of Biologically Active Heterocmentioning

confidence: 99%

“…Several drugs contain a quinazoline or quinazolinone ring, such as dacomitinib, alfusozine, bunazosin, Gefitinib, proquazone, letermovir, and afatinib [106]. In this context, Purkhosrowa et al [108] reported on the one-pot, solvent-and catalyst-free synthesis of new quinolone derivatives under ultrasonic irradiation and their vasorelaxant activity. To this end, the authors first reacted anthranilic acid, acetic anhydride, and anilines under ultrasonic irradiation to finalize the reaction conditions.…”

Section: Ultrasound-assisted Synthesis Of Biologically Active Heterocmentioning

confidence: 99%

Ultrasound for Drug Synthesis: A Green Approach

2020

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This last century, the development of new medicinal molecules represents a real breakthrough in terms of humans and animal life expectancy and quality of life. However, this success is tainted by negative environmental consequences. Indeed, the synthesis of drug candidates requires the use of many chemicals, solvents, and processes that are very hazardous, toxic, energy consuming, expensive, and generates a large amount of waste. Many large pharmaceutical companies have thus moved to using green chemistry practices for drug discovery, development, and manufacturing. One of them is the use of energy-efficient activation techniques, such as ultrasound. This review summarizes the latest most representative works published on the use of ultrasound for sustainable bioactive molecules synthesis.

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“…Quinazolines are fused heterocycles with a wide range of biological activities [ 1 , 2 ]. Nitrogen heterocycles exhibit diverse biological activities due to their similarities with many natural products.…”

Section: Introductionmentioning

confidence: 99%

Quinazolinones, the Winning Horse in Drug Discovery

2023

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Quinazolines are nitrogen-containing heterocycles that consist of a benzene ring fused with a pyrimidine ring. Quinazolinones, oxidized quinazolines, are promising compounds with a wide range of biological activities. In the pharmaceutical field, quinazolinones are the building blocks of more than 150 naturally occurring alkaloids isolated from different plants, microorganisms, and animals. Scientists give a continuous interest in this moiety due to their stability and relatively easy methods for preparation. Their lipophilicity is another reason for this interest as it helps quinazolinones in penetration through the blood–brain barrier which makes them suitable for targeting different central nervous system diseases. Various modifications to the substitutions around the quinazolinone system changed their biological activity significantly due to changes in their physicochemical properties. Structure–activity relationship (SAR) studies of quinazolinone revealed that positions 2, 6, and 8 of the ring systems are significant for different pharmacological activities. In addition, it has been suggested that the addition of different heterocyclic moieties at position 3 could increase activity. In this review, we will highlight the chemical properties of quinazolinones, including their chemical reactions and different methods for their preparation. Moreover, we will try to modify some of the old SAR studies according to their updated biological activities in the last twelve years.

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Implication of Quinazoline-4(3H)-ones in Medicinal Chemistry: A Brief Review

Cited by 23 publications

References 0 publications

Phytochemicals: Potential Lead Molecules for MDR Reversal

Phytochemicals: Potential Lead Molecules for MDR Reversal

Ultrasound for Drug Synthesis: A Green Approach

Quinazolinones, the Winning Horse in Drug Discovery

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