Disubstituted 4(3H) Quinazolones: A Novel Class of Antitumor Agents

Abstract

A series of disubstituted 4(3H) quinazolines were designed for potential application in tumors. Firstly, N-benzoyl anthranilic acid is formed, which undergoes cyclization in the presence of pyridine. Subsequently, nucleophilic attack by semicarbazide on the carbonyl carbon gives 2-substituted 3-carbamido 4(3H) quinazolones, which gives final compound with appropriate substitution. The final as well as intermediate products were confirmed by NMR, FT-IR, and mass spectrometry. In vitro toxicity was performed with different cell lines and showed that the connection of hydrophilic styryl to quinazoline moiety increases its efficacy.

Synthesis and In Vitro Evaluation of N‐Aryl Pyrido‐Quinazolines Derivatives as Potent Epidermal Growth Factor Receptor Inhibitors

“…Kinase reaction was quenched by removal of the reaction mixture and then the wells were washed with washing buffer for three times. Phosphorylated tyrosine substrate was blocked in PBS containing 3% BSA for 30 min, washed with washing buffer (PBS containing 0.1% Tween 20) for 3.74 (s, 3H, -OCH 3 ) 4.32 (d, 2H, -CH 2 ) 6.6 (s, 1H, -NH) 6.9 (d, 1H, -NH) 7.10-7.90 (m, 16H, ArH) three times, detected by adding antiphosphotyrosine antibody for 1 h. Then antibody was removed, and wells were washed with washing buffer for three times. The optical density was measured at 450 nm by an ELISA reader.…”

“…The quinazoline skeletons, present in a variety of biologically active compounds, are pharmacologically very attractive as reflected by activity in various assays. They are well known for a wide range of biological properties, including hypnotic, sedative, analgesic, anticonvulsant, antibacterial, antidiabetic, anti-inflammatory, and antitumor (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11). They also demonstrate several other useful and interesting properties such as hypertensive adrenergic blocker, selective phosphodiesterase inhibitor, against prostate disorders, dihydrofolate reductase inhibitor (12)(13)(14)(15)(16)(17)(18)(19)(20), etc.…”

The 18-kDa Translocator Protein PET Tracers as a Diagnostic Marker for Neuroinflammation: Development and Current Standing

“…4 The continuous increase in these diseases poses major health concerns throughout the globe, requiring more innovative and more selective radioprobes for diagnosis. 5,6 Apart from the neuroinflammation, pathophysiologic participation of TSPO is also briefly reported in cardiovascular situations in peripheral sterile inflammatory disorders (PSIDs). 7,8 Structure and Functions of 18 kDa TSPO.…”

Synthesis, Analytical Analysis, and Medicinal Aspect of Novel Benzimidazoles and their Metal Complexes

“…Benzimidazole analogs are known to be pharmacologically active and find their application in the treatment of various medical applications such as epilepsy, diabetics, and antifertility . Recently, many researches elucidated that benzimidazole analogs can be suitably modified by the introduction of different heterocyclic moieties to exhibit a broad spectrum of biologic activities such as potent anticancerous and microbial activities . Keeping this factor in our mind, we have modified benzimidazole analogs in such a way that would bring them into preferred orientation.…”