An overview of the biological evaluation of selected nitrogen-containing heterocycle medicinal chemistry compounds

O Ebenezer, MA Jordaan, G Carena, T Bono… - International Journal of …, 2022 - mdpi.com
Heterocyclic compounds are a class of compounds of natural origin with favorable
properties and hence have major pharmaceutical significance. They have an exceptional …

Designing strategies, structural activity relationship and biological activity of recently developed nitrogen containing heterocyclic compounds as epidermal growth …

R Pal, G Teli, GSP Matada, PS Dhiwar - Journal of Molecular Structure, 2023 - Elsevier
Cancer cells have the ability of dysregulation and autonomous proliferation due to
unchecked production of definite molecules. These molecules are involved in the cell growth …

An outlook of docking analysis and structure-activity relationship of pyrimidine-based analogues as EGFR inhibitors against non-small cell lung cancer (NSCLC)

R Pal, G Teli, S Sengupta, L Maji… - Journal of …, 2023 - Taylor & Francis
Almost 80% of lung cancer diagnoses each year correspond to non-small cell lung cancer
(NSCLC). The percentage of NSCLC with EGFR overexpression ranges from 40% to 89 …

Pyrazolo[3,4‐d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities

AE Kassab - Archiv der Pharmazie, 2023 - Wiley Online Library
Abstract The pyrazolo [3, 4‐d] pyrimidine core has received a lot of interest from the
medicinal chemistry community as a promising framework for drug design and discovery. It …

Novel pyrazolo [3, 4-d] pyrimidine derivatives: design, synthesis, anticancer evaluation, VEGFR-2 inhibition, and antiangiogenic activity

AM Abdelhamed, RA Hassan, HH Kadry… - RSC Medicinal …, 2023 - pubs.rsc.org
A novel series of 12 pyrazolo [3, 4-d] pyrimidine derivatives were created and evaluated in
vitro for their antiproliferative activity against the NCI 60 human tumor cell line panel …

Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

R Pal, G Teli, G Swamy Purawarga Matada… - …, 2023 - Wiley Online Library
Cancer is a wide collection of diseases and among the numerous pathways involved in
cancer pathogenesis, pathway involving epidermal growth factor receptor (EGFR) is one of …

Design, synthesis, biological evaluation, in silico ADME prediction and molecular docking of pyrazole-benzamides as multitargeting protien kinase inhibitors

NA Khaled, NS Ahmed, AZ Abdelazem… - Journal of Molecular …, 2023 - Elsevier
In the present study, N-(1-(2-bromobenzoyl)-4-cyano-1H-pyrazol-5-yl) halogenated
benzamides (5a-h) were prepared and evaluated for their in vitro anticancer activity against …

Novel Pyrimidine-5-Carbonitriles as potential apoptotic and antiproliferative agents by dual inhibition of EGFRWT/T790M and PI3k enzymes; Design, Synthesis …

N Reda, KO Mohamed, K Abdou, AA Helwa… - Bioorganic …, 2024 - Elsevier
Abstract A new series of 6-(4-fluorophenyl)-2-(methylthio) pyrimidine-5-carbonitrile
derivatives were designed and synthesized as EGFR/PI3K dual inhibitors, and potential …

In-Silico Investigation of Osimertinib Based Compounds as Potential Double Mutant EGFR Kinase Inhibitors Against H1975 Cell Line: Integrating QSAR Modeling …

S El Bahi, M Boutalaka, M Alaqarbeh, MA El Alaouy… - Chemistry Africa, 2024 - Springer
Epidermal growth factor receptor (EGFR) inhibitors have been proven as a high-potential
therapeutic target for treating advanced non-small-cell lung cancer (NSCLC). However …

Synthesis and bioassay of 3-Aryl -1-(pyridin-4-yl)benzo[4,5]imidazo[1,2-d][1,2,4]- triazin-4(3H)-ones as anti-cancer agents

BA Thaher, I Al-Masri, K Wahedy, R Morjan… - Naunyn-Schmiedeberg's …, 2023 - Springer
Abstract Four novel 3-Aryl-1-(pyridin-4-yl) benzo [4, 5] imidazo [1, 2-d][1, 2, 4]-triazin-4 (3H)-
ones derivatives (C1 to C4) have been designed, synthesized, and evaluated for their …