[HTML][HTML] The regulations of telomerase reverse transcriptase (TERT) in cancer

M Liu, Y Zhang, Y Jian, L Gu, D Zhang, H Zhou… - Cell Death & …, 2024 - nature.com
Abnormal activation of telomerase occurs in most cancer types, which facilitates escaping
from cell senescence. As the key component of telomerase, telomerase reverse …

Novel fused imidazotriazines acting as promising top. II inhibitors and apoptotic inducers with greater selectivity against head and neck tumors: Design, synthesis, and …

AA Al-Karmalawy, M Rashed, M Sharaky… - European Journal of …, 2023 - Elsevier
Although the great effectiveness of doxorubicin (Dox) in the treatment of many types of
tumors, it showed limited effectiveness against the head and neck squamous cell carcinoma …

Lead optimization of BIBR1591 to improve its telomerase inhibitory activity: design and synthesis of novel four chemical series with in silico, in vitro, and in vivo …

AA Al-Karmalawy, MHA Mousa… - Journal of Medicinal …, 2023 - ACS Publications
Herein, modifications to the previously reported BIBR1591 were conducted to obtain
bioisosteric candidates with improved activities. The% inhibition of the newly afforded …

Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic …

S El-Kalyoubi, MM Khalifa, MT Abo-Elfadl… - Journal of enzyme …, 2023 - Taylor & Francis
A new wave of dual Topo I/II inhibitors was designed and synthesised via the hybridisation
of spirooxindoles and pyrimidines. In situ selenium nanoparticles (SeNPs) for some …

[HTML][HTML] Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis …

SM Al-Muntaser, AA Al-Karmalawy, AM El-Naggar… - RSC …, 2023 - pubs.rsc.org
In this article, we continued our previous effort to develop new selective anticancer
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …

Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …

Discovery of novel pyridazine-tethered sulfonamides as carbonic anhydrase II inhibitors for the management of glaucoma

HO Tawfik, MM Saleh, A Ammara… - Journal of Medicinal …, 2024 - ACS Publications
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …

Development of new thieno [2, 3-d] pyrimidines as dual EGFR and STAT3 inhibitors endowed with anticancer and pro-apoptotic activities

HA Elsebaie, TF El-Moselhy, EA El-Bastawissy… - Bioorganic …, 2024 - Elsevier
In part due to the resilience of cellular feedback pathways that develop therapeutic
resistance to targeting the EGFR alone, using EGFR inhibitors alone was demonstrated to …

Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and …

F Farouk, AA Elmaaty, A Elkamhawy… - Journal of Enzyme …, 2023 - Taylor & Francis
Abstract Topoisomerase II (TOP-2) is a promising molecular target for cancer therapy.
Numerous antibiotics could interact with biologically relevant macromolecules and provoke …

Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In …

SM Hefny, TF El-Moselhy, N El-Din… - Journal of Medicinal …, 2024 - ACS Publications
A dual-targeting approach is predicted to yield better cancer therapy outcomes.
Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed and …