Occurrence of morpholine in central nervous system drug discovery

E Lenci, L Calugi, A Trabocchi - ACS Chemical Neuroscience, 2021 - ACS Publications
Developing drugs for the central nervous system (CNS) requires fine chemical modifications,
as a strict balance between size and lipophilicity is necessary to improve the permeability …

The chemo-and regioselectivity of the cyclization of thiosemicarbazides with haloacetic acids and their derivatives

AN Izmest'ev, AА Streltsov, AN Kravchenko… - Chemistry of …, 2022 - Springer
The Chemo- and Regioselectivity of the Cyclization of Thiosemicarbazides with Haloacetic Acids
and their Derivatives | Chemistry of Heterocyclic Compounds Skip to main content SpringerLink …

Design, synthesis, biological assessment, and in-silico studies of 1, 2, 4-triazolo [1, 5-a] pyrimidine derivatives as tubulin polymerization inhibitors

HS Mohamed, NH Amin, MT El-Saadi… - Bioorganic …, 2022 - Elsevier
Abstract A series of 1, 2, 4-triazolo [1, 5-a] pyrimidine derivatives have been designed and
synthesized as combretastatin CA-4 analogs. They were screened for anticancer and tubulin …

Design, synthesis and cytotoxicity screening of new synthesized pyrimidine-5-carbonitrile derivatives showing marked apoptotic effect

I Zaki, RE Masoud, MMS Hamoud, OAA Ali… - Journal of Molecular …, 2022 - Elsevier
A new series of pyrimidine-5-carbonitriles has been designed and synthesized as potent
anticancer agents. Pyrimidine-5-carbonitriles 2-6d have been assessed for their cytotoxic …

Design, synthesis and molecular docking study of new pyrimidine-based hydrazones with selective anti-proliferative activity against MCF-7 and MDA-MB-231 human …

WA Badawi, M Samir, HM Fathy, TM Okda… - Bioorganic …, 2023 - Elsevier
Efforts were directed on the design, synthesis and evaluation of the anticancer activity of
some pyrimidine-based hydrazones against two breast cancer cell lines, MCF-7 and MDA …

[HTML][HTML] Discovery of YS-363 as a highly potent, selective, and orally efficacious EGFR inhibitor

P He, J Jing, L Du, X Zhang, Y Ren, H Yang… - Biomedicine & …, 2023 - Elsevier
Abstract The Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) are
the standard first-line therapy for EGFR-mutated NSCLC. However, long-term clinical …

Novel antiproliferative agents bearing morpholinopyrimidine scaffold as PI3K inhibitors and apoptosis inducers; design, synthesis and molecular docking

AA Helwa, NM El-Dydamony, RA Radwan… - Bioorganic …, 2020 - Elsevier
Two series of novel morpholinopyrimidine derivatives were synthesized and screened for
their in-vitro cytotoxic activity against 60 tumor cell line by the National Cancer Institute, USA …

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFR WT/COX-2 inhibitors with docking studies

N Reda, A Elshewy, HI El-Askary, KO Mohamed… - RSC …, 2023 - pubs.rsc.org
A novel series of pyrimidine-5-carbonitrile derivatives was designed, synthesized, then
evaluated for their cytotoxic activity as novel anti-cancer with dual EGFRWT/COX-2 …

Pyrimidines as Anticancer and Antiviral: Synthesis & Reactions (A Review)

S Fatahala, M Mohamed, M Khodair… - Journal of Advanced …, 2022 - journals.ekb.eg
Background: The interest of many medicinal and organic chemists has been attracted to the
synthesis of pyrimidines and their analogues due to their highly biological and medicinal …

Virtual screening identifies tipranavir as a SIRT1 inhibitor with anti-hepatocarcinoma effect

Y Shen, Q Zhang, L Zhang, J Wang, M Shu… - Future Medicinal …, 2023 - Taylor & Francis
Aim: To identify novel inhibitors of SIRT1 and to understand their mechanism of action in
hepatocellular carcinoma. Materials & methods: Molecular docking and dynamic simulations …