[HTML][HTML] Vascular endothelial growth factor receptor (VEGFR-2)/KDR inhibitors: medicinal chemistry perspective
SJ Modi, VM Kulkarni - Medicine in Drug Discovery, 2019 - Elsevier
New blood vessels formation from the existing vasculature is called angiogenesis. It is an
essential physiological process for the growth of cells, tissue repair, wound healing, and …
essential physiological process for the growth of cells, tissue repair, wound healing, and …
Click Chemistry and Targeted Degradation: A Winning Combination for Medicinal Chemists?
A Pasieka, E Diamanti, E Uliassi… - …, 2023 - Wiley Online Library
Click chemistry is universally recognized as a powerful strategy for the fast and precise
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
Design, synthesis and evaluation of novel thienopyrimidine-based agents bearing diaryl urea functionality as potential inhibitors of angiogenesis
A Faraji, TO Bakhshaiesh, Z Hasanvand… - European Journal of …, 2021 - Elsevier
Inhibition of angiogenesis is a promising strategy for the treatment of cancer. Herein, we
describe the design and synthesis of thieno [2, 3-d] pyrimidine-1, 3, 4-thiadiazole-aryl urea …
describe the design and synthesis of thieno [2, 3-d] pyrimidine-1, 3, 4-thiadiazole-aryl urea …
Facile synthesis, structural activity relationship, molecular modeling and in vitro biological evaluation of new urea derivatives with incorporated isoxazole and thiazole …
FM Sroor, AM Abdelmoniem, IA Abdelhamid - ChemistrySelect, 2019 - Wiley Online Library
A new series of isoxazolyl and thiazolyl urea derivatives was synthesized, fully characterized
and evaluated in vitro as anticancer agents. The chemistry involves a facile protocol for the …
and evaluated in vitro as anticancer agents. The chemistry involves a facile protocol for the …
Discovery of novel PROTACs based on multi-targeted angiogenesis inhibitors
R Si, P Hai, Y Zheng, N Liu, J Wang, Q Zhang… - Bioorganic & Medicinal …, 2023 - Elsevier
Anti-angiogenesis has been proved to be an effective strategy for the treatment of tumors.
Anti-angiogenic drugs had achieved certain therapeutic effects. However, drug resistance …
Anti-angiogenic drugs had achieved certain therapeutic effects. However, drug resistance …
Discovery of novel anti-angiogenesis agents. Part 11: development of PROTACs based on active molecules with potency of promoting vascular normalization
Y Shan, R Si, J Wang, Q Zhang, J Li, Y Ma… - European Journal of …, 2020 - Elsevier
Our recent investigation is focused on the discovery of anti-angiogenesis agents. Vascular
normalization induced by anti-angiogenic agent appears to be a promising strategy. We …
normalization induced by anti-angiogenic agent appears to be a promising strategy. We …
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors
Y Sun, Y Shan, C Li, R Si, X Pan, B Wang… - European Journal of …, 2017 - Elsevier
Abstract VEGFR-2, TIE-2, and EphB4 are essential for both angiogenesis and
tumorigenesis. Herein, we designed and prepared three classes of multi-target inhibitors …
tumorigenesis. Herein, we designed and prepared three classes of multi-target inhibitors …
[HTML][HTML] Discovery and evaluation of triple inhibitors of VEGFR-2, TIE-2 and EphB4 as anti-angiogenic and anti-cancer agents
Receptor tyrosine kinases (RTKs), especially VEGFR-2, TIE-2, and EphB4, play a crucial
role in both angiogenesis and tumorigenesis. Moreover, complexity and heterogeneity of …
role in both angiogenesis and tumorigenesis. Moreover, complexity and heterogeneity of …
Novel pyrazolopyridine derivatives as potential angiogenesis inhibitors: Synthesis, biological evaluation and transcriptome-based mechanistic analysis
M Michailidou, V Giannouli, V Kotsikoris… - European Journal of …, 2016 - Elsevier
Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly
selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed …
selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed …
Discovery of novel anti-angiogenesis agents. Part 6: Multi-targeted RTK inhibitors
L Zhang, Y Shan, C Li, Y Sun, P Su, J Wang, L Li… - European Journal of …, 2017 - Elsevier
Angiogenesis is modulated by a multitude of pro-angiogenic factors including VEGFR-2, Tie-
2, and EphB4. Moreover, their crosstalk also had been well elaborated. We have identified …
2, and EphB4. Moreover, their crosstalk also had been well elaborated. We have identified …