Bioactive pyrrole-based compounds with target selectivity

GL Petri, V Spano, R Spatola, R Holl… - European journal of …, 2020 - Elsevier
The discovery of novel synthetic compounds with drug-like properties is an ongoing
challenge in medicinal chemistry. Natural products have inspired the synthesis of …

[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 …

Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors

AE Abdallah, RR Mabrouk, MMS Al Ward… - Journal of enzyme …, 2022 - Taylor & Francis
Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric
features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised …

In silico screening and anticancer-apoptotic evaluation of newly synthesized thienopyrimidine/sulfonamide hybrids

EI Elmongy, FA Binjubair, OY Alshehri… - International Journal of …, 2023 - mdpi.com
This work describes the design and synthesis of new hybrids of thienopyrimidine and
sulfonamides. The binding affinity of the prepared compounds to FGFR-1 enzyme and …

New fluorinated diarylureas linked to pyrrolo [2, 3-d] pyrimidine scaffold as VEGFR-2 inhibitors: Molecular docking and biological evaluation

M Adel, KAM Abouzid - Bioorganic Chemistry, 2022 - Elsevier
Abstract A series of pyrrolo [2, 3-d] pyrimidine linked to diarylureas were previously
discovered by our group as sorafenib fused congeners, which were endowed with more …

3D-QSAR pharmacophore modelling, virtual screening and docking studies for lead discovery of a novel scaffold for VEGFR 2 inhibitors: design, synthesis and …

MK Sobhy, S Mowafy, DS Lasheen, NA Farag… - Bioorganic …, 2019 - Elsevier
Abstract A series of novel 6, 7-dihydro-5H-cyclopenta [d] pyrimidine derivatives was
successfully designed, synthesized and evaluated as a new chemical scaffold with vascular …

Double-edged swords: diaryl pyrazoline thiazolidinediones synchronously targeting cancer epigenetics and angiogenesis

N Upadhyay, K Tilekar, S Safuan, AP Kumar… - Bioorganic …, 2021 - Elsevier
In the present study, two novel series of compounds incorporating naphthyl and pyridyl
linker were synthesized and biological assays revealed 5-((6-(2-(5-(2-chlorophenyl)-3-(4 …

Scaffold hopping and redesign approaches for quinazoline based urea derivatives as potent VEGFR-2 inhibitors

SR Abd El Hadi, DS Lasheen, DH Soliman… - Bioorganic …, 2020 - Elsevier
In our attempt to discover effective anticancer agents, three series of novel quinazoline-
based compounds have been designed, synthesized and tested as VEGFR-2 inhibitors. Five …

Multi-target weapons: diaryl-pyrazoline thiazolidinediones simultaneously targeting VEGFR-2 and HDAC cancer hallmarks

N Upadhyay, K Tilekar, S Safuan, AP Kumar… - RSC Medicinal …, 2021 - pubs.rsc.org
In anticancer drug discovery, multi-targeting compounds have been beneficial due to their
advantages over single-targeting compounds. For instance, VEGFR-2 has a crucial role in …

An appraisal on synthetic and medicinal aspects of fused pyrimidines as anti neoplastic agents

I Rani, N Kaur, A Goyal… - Anti-Cancer Agents in …, 2023 - ingentaconnect.com
Heterocyclic compounds are recognized to possess a high grade of structural diversity and a
broad spectrum of therapeutic properties. About two-thirds of the New Chemical Entities …