Tail-approach based design, synthesis, and cytotoxic evaluation of novel disubstituted and trisubstituted 1,3-thiazole benzenesulfonamide derivatives with suggested carbonic anhydrase IX inhibition mechanism

Samir Bondock, Tallah Albarqi, Mohamed Abboud, Tamer Nasr, Nada M. Mohamed and Moaz M. Abdou

RSC Adv., 2023,13, 24003-24022

Abstract

A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzenesulfonamide was designed following the tail approach as possible hCAIX inhibitors.

Novel asymmetrical azines appending 1,3,4-thiadiazole sulfonamide: synthesis, molecular structure analyses, in silico ADME, and cytotoxic effect

Samir Bondock, Tallah Albarqi, Ibrahim A. Shaaban and Moaz M. Abdou

RSC Adv., 2023,13, 10353-10366

From themed collection: 2023 RSC Advances Popular Advances Collection

Abstract

Toward finding potential and novel anticancer agents, we designed and prepared novel differently substituted unsymmetrical azine-modified thiadiazole sulfonamide derivatives using the “combi-targeting approach”.

New nicotinamide–thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and in silico and in vitro evaluation

Walid E. Elgammal, Hazem Elkady, Reda G. Yousef, Wagdy M. Eldehna, Dalal Z. Husein, Fatma G. Amin, Bshra A. Alsfouk, Eslam B. Elkaeed, Ibrahim H. Eissa and Ahmed M. Metwaly

RSC Adv., 2025,15, 14477-14498

Abstract

Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development.

Rationale design and synthesis of new apoptotic thiadiazole derivatives targeting VEGFR-2: computational and in vitro studies

Walid E. Elgammal, Hazem Elkady, Hazem A. Mahdy, Dalal Z. Husein, Aisha A. Alsfouk, Bshra A. Alsfouk, Ibrahim M. Ibrahim, Eslam B. Elkaeed, Ahmed M. Metwaly and Ibrahim H. Eissa

RSC Adv., 2023,13, 35853-35876

Abstract

This work presents the synthesis and in vitro, and in silico analyses of new thiadiazole derivatives that are designed to mimic the pharmacophoric characteristics of vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors.

Discovery of thieno[2,3-d]pyrimidine-based dual Aurora B/VEGFR-2 inhibitors with potent anticancer activity: molecular docking, mechanistic studies, and in vivo validation in a breast cancer model

Hamed W. El-Shafey, Abdelrahman Hamdi, Mohamed R. Elnagar, Sahar M. Gebril, Abdullah Haikal, Adel S. El-Azab, Simone Brogi, Ibrahim A. Al-Suwaidan and Alaa A.-M. Abdel-Aziz

RSC Adv., 2026,16, 21079-21098

Abstract

Breast cancer continues to be the most common malignancy in women and a major contributor of cancer-related mortality, emphasizing the need for novel therapeutic agents.