Evaluation of the use of therapeutic peptides for cancer treatment
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 …
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 …
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 …
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 …
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 …
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 …
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?
The ATP site of kinases displays remarkable conformational flexibility when accommodating
chemically diverse small molecule inhibitors. The so-called activation segment, whose …
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 …
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 …
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
Eleven new quinoxaline derivatives were designed and synthesized as modified VEGFR-2
inhibitors of our previous work. The synthesized compounds were tested against three …
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 …
was synthesised. The antiproliferative effects of these compounds were estimated against …