A century-old one-pot multicomponent Biginelli reaction products still finds a niche in drug discoveries: Synthesis, mechanistic studies and diverse biological activities …

S Faizan, TF Roohi, RM Raju, Y Sivamani… - Journal of Molecular …, 2023 - Elsevier
One of the largest classes of organic molecules are dihydropyrimidines and its derivatives.
They are widely used in a variety of pharmacological and industrial applications. Their …

Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …

Medicinal perspective of a promising scaffold–dihydropyrimidinones: A review

BH Sarvaiya, PI Vaja, NA Paghdar… - Journal of Heterocyclic …, 2024 - Wiley Online Library
Dihydropyrimidinones (DHMPs) are the most important pharmacophore in Medicinal
Chemistry. The synthetic approach for deriving DHMPs involves the Biginelli reaction or a …

Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R)

MG Abo Al-Hamd, HO Tawfik, O Abdullah… - Journal of Enzyme …, 2023 - Taylor & Francis
Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new
series of anticancer agents. Thirty-two new compounds were synthesised where x-ray …

[HTML][HTML] Synthesis, evaluation of the cytotoxicity, apoptosis induction in AGS cell line and gene expression and molecular modeling studies of novel …

S Sepehri, Y Panahi, D Abbasi, M Jafari… - Arabian Journal of …, 2024 - Elsevier
Cancer is a complex disease that remains a leading cause of death worldwide owing to the
lack of effective and efficient drugs. Compounds known as tetrahydropyrmidine have shown …

Revisiting ageless antiques; synthesis, biological evaluation, docking simulation and mechanistic insights of 1, 4-Dihydropyridines as anticancer agents

PA Sidhom, E El-Bastawissy, AA Salama… - Bioorganic …, 2021 - Elsevier
The historic DHP nucleus was serendipitously discovered by Arthur Hantzsch about 130
years ago and is still considered a hidden treasure for various pharmacological activities …

Negative modulation of the angiogenic cascade induced by allosteric kinesin Eg5 inhibitors in a gastric adenocarcinoma in vitro model

A Ricci, M Gallorini, D Del Bufalo, A Cataldi… - Molecules, 2022 - mdpi.com
Eg5 is a kinesin essential in bipolar spindle formation, overexpressed in tumours, thus
representing a new target in cancer therapy. We aimed at evaluating the anti-cancer activity …

Design, synthesis, molecular dynamics simulation, MM/GBSA studies and kinesin spindle protein inhibitory evaluation of some 4-aminoquinoline hybrids

SD Ranade, SG Alegaon… - … Biology and Chemistry, 2023 - Elsevier
The discovery of novel chemotherapeutic agents is always challenging for researchers in
industry and academia. Among the recent promising anticancer therapeutic targets, an …

Synthesis of substituted hexahydro-2H-chromeno[4,3-d]pyrimidine-2,5-diones and their modification at the hydroxy group

ES Makarova, MV Kabanova, SI Filimonov… - Russian Chemical …, 2022 - Springer
Synthesis of substituted hexahydro-2H-chromeno[4,3-d]pyrimidine-2,5-diones and their
modification at the hydroxy group Page 1 Russian Chemical Bulletin, Vol. 71, No. 5, pp …

Microwave-accelerated multicomponent synthesis and X-ray characterization of novel benzothiadiazinone dioxide derivatives, analogues of Monastrol

A Bouzina, M Berredjem, B Belhani, S Bouacida… - Research on Chemical …, 2021 - Springer
We demonstrate here a rapid and comfortable synthetic sequence to benzothiadiazinone
dioxide (six-membered cyclic sulfamide) derivatives, analogues of Monastrol, which is …