Development of indole hybrids for potential lung cancer treatment-part I: nitrogen-containing six-membered aromatic heterocycles

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 17

Published: March 29, 2025

Lung cancer is the most prevalent invasive malignancy and leading cause of cancer-related death. Chemotherapy vital for lung therapy, but multidrug resistance responsible majority fatalities, creating an imperative demand to develop novel chemotherapeutics. Indole a valuable anti-lung pharmacophore since its derivatives could act on cells through various mechanisms. Notably, indole hybrids inhibit multiple targets simultaneously have potential overcome shortcomings traditional Moreover, many such as indole-pyrimidine hybrid osimertinib indole-hydroxamic acid panobinostat, are either under clinical evaluations or already been approved therapy. This indicates that rational design represents highly prospective approach development new chemotherapeutic agents. review focuses exploring therapeutic delves into their action mechanisms well structure-activity correlations, covering articles published between 2021 present. The ultimate goal offer foundation in future.

Language: Английский

An insight into the in vivo antitumor therapeutic potential of indole-(fused) pyri(mi)dine hybrids

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 19

Published: May 14, 2025

Cancer can invade and destroy any part of the body, representing a grand social, public health, economic challenge. Chemotherapy plays crucial role in cancer treatment, recent decades, hundreds anticancer chemotherapeutics have been introduced. Nevertheless, multidrug resistance side effects are main obstacles to successful therapy, highlighting pressing requirement for development new address above issues. Indole hybrids not only potential surmount drug adverse caused by individual components but also enhance efficacy improve pharmacokinetic characteristics since hybrid molecules concurrently regulate multiple targets within cells. Moreover, numerous indole exemplified mobocertinib (indole-pyrimidine hybrid) osimertinib (indole-quinazoline already utilized clinical treatment. Therefore, emerged as valuable scaffolds treatment eradication cancer. This review aims elucidate current landscape indole-(fused) pyri(mi)dine hybrids, including indole-quinolines/quinolinones, indole-pyridines, indole-pyrimidines, indole-fused pyrimidines, with vivo antitumor therapeutic potential, offering effective candidates in-depth preclinical evaluations, encompassing articles published from 2021 onward.

Language: Английский