Design and synthesis of hybrid compounds as novel drugs and medicines

AH Alkhzem, TJ Woodman, IS Blagbrough - RSC advances, 2022 - pubs.rsc.org
The development of highly effective conjugate chemistry approaches is a way to improve the
quality of drugs and of medicines. The aim of this paper is to highlight and review such …

Triple targeting of mutant EGFRL858R/T790M, COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti …

H Kothayer, S Rezq, AS Abdelkhalek… - Journal of Enzyme …, 2023 - Taylor & Francis
We designed and synthesised novel quinazolinone tethered phenyl urea derivatives (6a–p)
that triple target the double mutant EGFRL858R/T790M, COX-2, and 15-LOX. Compounds …

Tissue distribution and endocrine disruption effects of chronic exposure to pharmaceuticals and personal care products mixture at environmentally relevant …

N Hamid, M Junaid, R Manzoor, JJ Duan, M Lv, N Xu… - Aquatic Toxicology, 2022 - Elsevier
Pharmaceuticals and personal care products (PPCPs) as emerging contaminants are
ubiquitously present in the aquatic environment. Using in vivo and in silico techniques, this …

Optimization of pyrrolizine-based Schiff bases with 4-thiazolidinone motif: Design, synthesis and investigation of cytotoxicity and anti-inflammatory potency

AM Shawky, MAS Abourehab, AN Abdalla… - European journal of …, 2020 - Elsevier
Two new series of pyrrolizine-5-carboxamides were synthesized and evaluated for their
anticancer and anti-inflammatory activities. The new compounds exhibited potent cytotoxicity …

Synthesis and anti-inflammatory evaluation of new chalcone derivatives bearing bispiperazine linker as IL-1β inhibitors

YL Tang, X Zheng, Y Qi, XJ Pu, B Liu, X Zhang, XS Li… - Bioorganic …, 2020 - Elsevier
In this work, a series of novel chalcone derivatives bearing bispiperazine linker have been
synthesized and in vitro anti-inflammatory, cytotoxic activity and anti-inflammatory …

Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

N Ahmadi, M Rincón, M Silva-Abreu, L Sosa… - Gels, 2023 - mdpi.com
Pranoprofen (PRA)-loaded nanostructured lipid carriers (NLC) have been dispersed into
blank gels composed of 1% of Carbomer 940 (PRA-NLC-Car) and 3% of Sepigel® 305 …

Discovery of novel pyrazole based Urea/Thiourea derivatives as multiple targeting VEGFR-2, EGFRWT, EGFRT790M tyrosine kinases and COX-2 Inhibitors, with anti …

WAA Fadaly, MTM Nemr, NM Kahk - Bioorganic Chemistry, 2024 - Elsevier
A novel series of pyrazole derivatives with urea/thiourea scaffolds 16a-l as hybrid
sorafenib/erlotinib/celecoxib analogs was designed, synthesized and tested for its VEGFR-2 …

Design, synthesis and biological evaluation of antitumor platinum (II) agents conjugated with non-steroidal anti-inflammatory drug species

J Zang, B Zhang, Y Wang, X Wang, S Gou - Bioorganic Chemistry, 2022 - Elsevier
As one of the key features of tumor, inflammation attracts much attention of many
researchers for antitumor study, in which non-steroidal anti-inflammatory drugs (NSAIDs) …

Synthesis of naproxen thiadiazole urea hybrids and determination of their anti-melanoma, anti-migration, tyrosinase inhibitory activity, and molecular docking studies

BZ Kurt, Ö Altundağ, M Gökçe, U Cakmak… - Journal of Molecular …, 2024 - Elsevier
Novel sixteen naproxen urea compounds were synthesized bearing the thiadiazole ring.
Their inhibitory activities against tyrosinase were investigated. 3o was discovered to be the …

Ethyl benzoate bearing pyrrolizine/indolizine moieties: Design, synthesis and biological evaluation of anti-inflammatory and cytotoxic activities

KM Attalah, AN Abdalla, A Aslam, M Ahmed… - Bioorganic …, 2020 - Elsevier
Two new series of ethyl benzoate bearing pyrrolizine and indolizine moieties 8–11 were
synthesized and evaluated for their anti-inflammatory and anticancer activities. Among these …