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Pyrimidine containing epidermal growth factor receptor kinase inhibitors: Synthesis and biological evaluation
(Blackwell Publishing Ltd, 2017)
Structure-based design and synthesis of pyrimidine containing reversible epidermal growth factor receptor (EGFR) inhibitors 1a?d are reported. The compounds (1a?d) inhibited the EGFR kinase activity in vitro with IC50 range ...
Toward an Understanding of Structural Insights of Xanthine and Aldehyde Oxidases: An Overview of their Inhibitors and Role in Various Diseases
(John Wiley and Sons Inc., 2018)
Almost all drug molecules become the substrates for oxidoreductase enzymes, get metabolized into more hydrophilic products and eliminated from the body. These metabolites sometime may be more potent, active, inactive, or ...
Role of genomic alterations in HER2 positive breast carcinoma: Focus on susceptibility and trastuzumab-therapy
(Bentham Science Publishers B.V., 2017)
Background: Breast cancer is the most frequently diagnosed life-threatening malignancy among women, across the globe. HER2 positive is a distinct breast cancer subtype, on account of its unique biology and physiological ...
Synthetic versus enzymatic pictet-spengler reaction: An overview
(Bentham Science Publishers B.V., 2018)
Background: Pictet-Spengler reactions is an irreplaceable part of cyclization reaction leading to the formation of indispensable heterocyclic moieties including imidazole, benzoxazole, pyrrole, indole and others having ...
Association of CYP2C19*2 and ALDH1A1*1/*2 variants with disease outcome in breast cancer patients: results of a global screening array.
(Springer, 2018)
Cyclophosphamide and doxorubicin (adjuvant chemotherapy) are commonly used to treat breast cancer patients. Variation in the genes involved in pharmacodynamics and pharmacokinetics of these drugs plays an important role ...
Design, synthesis, biological evaluation of 3,5-diaryl-4,5-dihydro-1H-pyrazole carbaldehydes as non-purine xanthine oxidase inhibitors: Tracing the anticancer mechanism via xanthine oxidase inhibition
(Academic Press Inc., 2021-01-07)
Xanthine oxidase (XO) has been primarily targeted for the development of anti-hyperuriciemic /anti-gout agents as it catalyzes the conversion of xanthine and hypoxanthine into uric acid. XO overexpression in various cancer ...
Molecular Docking and In Vitro Anticancer Screening of Synthesized Arylthiazole linked 2H-indol-2-one Derivatives as VEGFR-2 Kinase Inhibitors
(Bentham Science Publishers, 2021-11-18)
Background: Indoline-2,3-dione comprises a leading course group of heterocycles endowed with appealing biological actions, including anticancer activity. There are significant justifications for exploring the anticancer ...
Flavonoids as P-glycoprotein inhibitors for multidrug resistance in cancer: an in-silico approach
(Taylor and Francis Ltd., 2022-09-19)
Cancer has become a leading cause of mortality due to non-communicable diseases after cardiovascular disease worldwide and is increasing day by day at a daunting pace. According to an estimate by 2040 there will be 28.4 ...
Rationalization of the activity Profile of Pyruvate Kinase Isozyme M2 (PKM2) Inhibitors using 3D QSAR
(Bentham Science Publishers, 2021-08-05)
Introduction: Pyruvate kinase isozyme M2 (PKM2) was observed to be overexpressed and play a key role in cell growth and cancer cells' metabolism. During the past years, phytochemicals have been developed as new treatment ...