Evaluation of the use of therapeutic peptides for cancer treatment

S Marqus, E Pirogova, TJ Piva - Journal of biomedical science, 2017 - Springer
Cancer along with cardiovascular disease are the main causes of death in the industrialised
countries around the World. Conventional cancer treatments are losing their therapeutic …

Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001–2011)

J Wang, M Sánchez-Roselló, JL Aceña… - Chemical …, 2014 - ACS Publications
1.1. Brief Historical Overview As expected from the fluorine position on the periodic table of
elements, it possesses some extreme properties, in particular, ultimate electronegativity and …

Design and synthesis of thiazolidine-2, 4-diones hybrids with 1, 2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: In-vitro anticancer evaluation …

MS Taghour, H Elkady, WM Eldehna… - Journal of Enzyme …, 2022 - Taylor & Francis
Abstract A thiazolidine-2, 4-dione nucleus was molecularly hybridised with the effective
antitumor moieties; 2-oxo-1, 2-dihydroquinoline and 2-oxoindoline to obtain new hybrids …

Making sense of large-scale kinase inhibitor bioactivity data sets: a comparative and integrative analysis

J Tang, A Szwajda, S Shakyawar, T Xu… - Journal of Chemical …, 2014 - ACS Publications
We carried out a systematic evaluation of target selectivity profiles across three recent large-
scale biochemical assays of kinase inhibitors and further compared these standardized …

Dual or multi-targeting inhibitors: The next generation anticancer agents

NM Raghavendra, D Pingili, S Kadasi, A Mettu… - European journal of …, 2018 - Elsevier
Dual-targeting/Multi-targeting of oncoproteins by a single drug molecule represents an
efficient, logical and alternative approach to drug combinations. An increasing interest in this …

Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?

Z Zhao, H Wu, L Wang, Y Liu, S Knapp, Q Liu… - ACS chemical …, 2014 - ACS Publications
The ATP site of kinases displays remarkable conformational flexibility when accommodating
chemically diverse small molecule inhibitors. The so-called activation segment, whose …

Discovery of thieno [2, 3-d] pyrimidine-based derivatives as potent VEGFR-2 kinase inhibitors and anti-cancer agents

SA El-Metwally, MM Abou-El-Regal, IH Eissa… - Bioorganic …, 2021 - Elsevier
Vascular endothelial growth factor-2 (VEGFR-2) is considered one of the most important
factors in tumor angiogenesis, and consequently a number of anticancer therapeutics have …

Drugging MYCN through an allosteric transition in Aurora kinase A

WC Gustafson, JG Meyerowitz, EA Nekritz, J Chen… - Cancer cell, 2014 - cell.com
MYC proteins are major drivers of cancer yet are considered undruggable because their
DNA binding domains are composed of two extended alpha helices with no apparent …

New quinoxaline-2 (1 H)-ones as potential VEGFR-2 inhibitors: Design, synthesis, molecular docking, ADMET profile and anti-proliferative evaluations

RG Yousef, HM Sakr, IH Eissa, ABM Mehany… - New Journal of …, 2021 - pubs.rsc.org
Eleven new quinoxaline derivatives were designed and synthesized as modified VEGFR-2
inhibitors of our previous work. The synthesized compounds were tested against three …

New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies

EB Elkaeed, MS Taghour, HA Mahdy… - Journal of Enzyme …, 2022 - Taylor & Francis
New quinoline and isatin derivatives having the main characteristics of VEGFR-2 inhibitors
was synthesised. The antiproliferative effects of these compounds were estimated against …