The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogencontaining heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. Various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

Belinostat is a histone deacetylase inhibitor used for the management of hematological malignancies and solid tumors. In the current study, stability-indicating ultra-performance liquid chromatogra...

In present study, a novel, simple, robust, stability-indicating, highly sensitive and specific reverse phase ultra-performance liquid chromatographic method was established and validated for the determination of ibrutinib using acquity charged surface hybrid C-18 (100 mm×2.1 mm, 1.7 μm) column with a mobile phase consisting of mixture of Eluent-A phosphate buffer, 0.1 % triethylamine, (pH 6.0) and Eluent-B acetonitrile with flow rate 0.3 ml min-1. The detection was monitored at 215 nm using photodiode array detector. Linearity was observed from 25 to 250 ng ml-1 (correlation of coefficient was 0.9999) with equation, y=100.1880x-130.8966. The observed limit of detection and limit of quantitation were 25 ng ml-1 and 50 ng ml-1 respectively. Ibrutinib was subjected to stress conditions comprising hydrolytic (acid, alkali and neutral), oxidative, photolytic and thermal degradation as per International council for harmonisation Q1 guidelines. The results showed that substantial degradation were observed in acid, base and peroxide degradation condition and resistant to neutral, photolytic and thermal degradation. This is first highly sensitive stability-indicating ultra-performance liquid chromatography method capable of separating ibrutinib and its ten degradation products at nano gram (ng) level. The method was validated as stated by International council for harmonisation guidelines.

Coronavirus 2019 (COVID-19) is caused by ‘severe acute respiratory syndrome coronavirus 2′ (SARS-CoV-2), first reported in Wuhan, China in December 2019, which eventually became a global disaster. Various key mediators have been reported in the pathogenesis of COVID-19. However, no effective pharmacological intervention has been available to combat COVID-19 complications. The present study screens nicotinamide riboside (NR) and nicotinamide mononucleotide (NMN) as potential inhibitors of this present generation coronavirus infection using an in-silico approach. The SARS-CoV-2 proteins (nucleocapsid, proteases, post-fusion core, phosphatase, endoriboruclease) and ACE-2 protein were selected. The 2D structure of nicotinamide ribonucleoside and nicotinamide ribonucleotide was drawn using ChemDraw 14.0 and saved in .cdx format. The results were analyzed using two parameters: full fitness energy and binding free energy (ΔG). The full fitness energy and estimated ΔG values from docking of NM, and NMN with selected SARS-CoV-2 target proteins, ADMET prediction and Target prediction indicate the interaction of NR and NMN in the treatment of COVID-19. Based on full fitness energy and estimated ΔG values from docking studies of NM and NAM with selected SARS-CoV-2 target proteins, ADME prediction, target prediction and toxicity prediction, we expect a possible therapeutic efficacy of NR in the treatment of COVID-19.