The anti‐breast cancer potential of indole/isatin hybrids

Abstract

Breast cancer (BC) is one of the most prevalent malignancies and the major contributor to cancer mortality in women globally, with a high degree of heterogeneity and a dismal prognosis. As drug resistance is responsible for most BC fatalities and advanced BC is currently considered incurable, finding innovative anti‐BC chemotherapeutics is urgently required. Indole and its analog isatin (indole‐1H‐2,3‐dione) are prominent pharmacophores in the development of novel medications, and their derivatives exhibit strong anticancer activities, also against BC. In particular, indole/isatin hybrids exhibit significant potency against BC including multidrug‐resistant forms and excellent selectivity by influencing a variety of biological targets associated with the disease, supplying helpful building blocks for the identification of potential new BC treatment options. This review includes articles from 2020 to the present and provides insights into the in vitro and in vivo anti‐BC potential, molecular mechanisms, and structure–activity relationships (SARs) of indole/isatin hybrids that may be helpful in the development of innovative anti‐BC chemotherapeutics.

Two-carbon tethered artemisinin–isatin hybrids: design, synthesis, anti-breast cancer potential, and in silico study

“…Hybrid molecules, generated by combining two or more molecule entities, could affect multiple targets to fight against various diseases including breast cancers ( Bérubé, 2016 ; Waseem and Ahmad, 2022 ; Wang et al, 2023a ). Artemisinin (ART) and its derivatives (dihydroartemisinin/DHA, artesunate, and artemether), from the traditional Chinese medicine drug, possess a unique peroxy bridge structure, and they could exert the anticancer effects through diverse mechanisms, inclusive of cell cycle inhibition, inhibition of tumor angiogenesis, promotion of DNA damage, and promotion of ferroptosis ( Zhang S. et al, 2022a ; Hu et al, 2022 ).…”