An insight on medicinal attributes of 1, 2, 4-triazoles

R Aggarwal, G Sumran - European journal of medicinal chemistry, 2020 - Elsevier
The present review aims to summarize the pharmacological profile of 1, 2, 4-triazole, one of
the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant …

Challenges and Opportunities in the Crusade of BRAF Inhibitors: From 2002 to 2022

AK Singh, P Sonawane, A Kumar, H Singh… - ACS …, 2023 - ACS Publications
Serine/threonine-protein kinase B-Raf (BRAF; RAF= rapidly accelerated fibrosarcoma) plays
an important role in the mitogen-activated protein kinase (MAPK) signaling cascade …

Synthesis, anticancer activity and molecular modeling studies of 1, 2, 4-triazole derivatives as EGFR inhibitors

HAM El-Sherief, BGM Youssif, SNA Bukhari… - European journal of …, 2018 - Elsevier
A series of novel compounds carrying 1, 2, 4-triazole scaffold were prepared and evaluated
for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (ad), and …

1, 5-diaryl-1, 2, 4-triazole ureas as new SLC-0111 analogues endowed with dual carbonic anhydrase and VEGFR-2 inhibitory activities

AE Elsawi, MM Elbadawi, A Nocentini… - Journal of Medicinal …, 2023 - ACS Publications
Presently, dual targeting by a single small molecule stands out as an effective cancer-
fighting weapon. Carbonic anhydrase (CA) and vascular-endothelial growth factor (VEGF) …

Design and synthesis of novel quinoline/chalcone/1, 2, 4-triazole hybrids as potent antiproliferative agent targeting EGFR and BRAFV600E kinases

AM Mohassab, HA Hassan, D Abdelhamid… - Bioorganic …, 2021 - Elsevier
New quinoline/chalcone hybrids containing 1, 2, 4-triazole moiety have been designed,
synthesized and their structures elucidated and confirmed by various spectroscopic …

DeepBSP—a machine learning method for accurate prediction of protein–ligand docking structures

J Bao, X He, JZH Zhang - Journal of chemical information and …, 2021 - ACS Publications
In recent years, machine-learning-based scoring functions have significantly improved the
scoring power. However, many of these methods do not perform well in distinguishing the …

Development of dual inhibitors targeting epidermal growth factor receptor in cancer therapy

L Tan, J Zhang, Y Wang, X Wang, Y Wang… - Journal of Medicinal …, 2022 - ACS Publications
Epidermal growth factor receptor (EGFR) is of great significance in mediating cell signaling
transduction and tumor behaviors. Currently, third-generation inhibitors of EGFR, especially …

Optimization and SAR investigation of novel 2, 3-dihydropyrazino [1, 2-a] indole-1, 4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent …

HAM Gomaa, ME Shaker, SI Alzarea, OM Hendawy… - Bioorganic …, 2022 - Elsevier
Using a single drug to treat cancer with dual-targeting is an unusual approach when
compared to other drug combinations. Dual-targeting agents were developed as a result of …

Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic …

FAM Mohamed, HAM Gomaa, OM Hendawy, AT Ali… - Bioorganic …, 2021 - Elsevier
New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide
derivatives has been designed, synthesized, and tested for antiproliferative activity against a …

Synthesis and biological evaluation of 3-amino-1, 2, 4-triazole derivatives as potential anticancer compounds

O Grytsai, O Valiashko, M Penco-Campillo, M Dufies… - Bioorganic …, 2020 - Elsevier
Two series of compounds carrying 3-amino-1, 2, 4-triazole scaffold were synthesized and
evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay …