Donepezil-based rational design of N-substituted quinazolinthioacetamide candidates as potential acetylcholine esterase inhibitors for the treatment of Alzheimer's disease: in vitro and in vivo studies

Ahmed A. Al-Karmalawy, Ahmed F. Mohamed, Heba Nasr Shalaby, Ayman Abo Elmaaty, Riham A. El-Shiekh, Mohamed A. Zeidan, Radwan Alnajjar, Abdullah Yahya Abdullah Alzahrani, Mohammed H. AL Mughram, Moataz A. Shaldam and Haytham O. Tawfik

RSC Med. Chem., 2025,16, 2078-2097

Abstract

Donepezil-based rational design of N-substituted quinazoline tethered thioacetamide as potential acetylcholine esterase inhibitors for the treatment of Alzheimer's disease.

Synthesis, ADMT prediction, and in vitro and in silico α-glucosidase inhibition evaluations of new quinoline–quinazolinone–thioacetamides

Sajedeh Safapoor, Mohammad Halimi, Minoo Khalili Ghomi, Milad Noori, Navid Dastyafteh, Shahrzad Javanshir, Samanesadat Hosseini, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Ensieh Nasli-Esfahani, Bagher Larijani, Azadeh Fakhrioliaei, Mohammad G. Dekamin, Maryam Mohammadi-Khanaposhtani and Mohammad Mahdavi

RSC Adv., 2023,13, 19243-19256

Abstract

In this work, a new series of quinoline–quinazolinone–thioacetamide derivatives 9a–p were designed using a combination of effective pharmacophores of the potent α-glucosidase inhibitors.

A scalable and eco-friendly total synthesis of poly(ADP-ribose) polymerase inhibitor Olaparib

Indranil Chatterjee, Deblina Roy and Gautam Panda

Green Chem., 2023,25, 9097-9102

Abstract

A scalable and eco-friendly total synthesis of PARP inhibitor.

Design, synthesis, anticancer evaluation, and in silico ADMET analysis of novel thalidomide analogs as promising immunomodulatory agents

Anas Ramadan Kotb, Abdallah E. Abdallah, Hazem Elkady, Ibrahim H. Eissa, Mohammed S. Taghour, Dina Abed Bakhotmah, Tamer M. Abdelghany and Mohamed Ayman El-Zahabi

RSC Adv., 2023,13, 10488-10502

Abstract

Novel thalidomide analogs as anticancer immunomodulatory agents.

S-Alkylated quinazolin-4(3H)-ones as dual EGFR/VEGFR-2 kinases inhibitors: design, synthesis, anticancer evaluation and docking study

Samar S. Tawfik, Abdelrahman Hamdi, Ahmed R. Ali, Abdullah A. Elgazar, Hamed W. El-Shafey, Adel S. El-Azab, Ahmed H. Bakheit, Mohamed M. Hefnawy, Hazem A. Ghabbour and Alaa A.-M. Abdel-Aziz

RSC Adv., 2024,14, 26325-26339

Abstract

Novel quinazolin-4(3H)-ones 4–27 were synthesized. Compounds 4, 11, and 20 showed potential anti-tumour activities. 4, 11, and 20 blocked EGFR/VEGFR-2 and triggered apoptosis. Compound 4 showed the most potent activity against EGFR/VEGFR-2.