Isatin Hybrids and Their Pharmacological Investigations

Abstract

Abstract:: Hybridization is an important strategy to design molecules that can be effectively used to treat fatal diseases known to mankind. Molecular hybrids and their pharmacological investigations aided to discover several potent isatin (Indole 2, 3 dione) derivatives with anti-HIV, antimalarial, antitubercular, antibacterial, and anticancer activities. Indole‐2,3‐dione and their derivatives have diverse pharmacological properties and have a prominent role in the discovery of new drugs. To understand the various approaches in designing new molecules based on isatin nucleus analysis of various pharmacophore hybrids, spacers/linkers between pharmacophores and isatin for hybridization and their biological activities is important. This review discusses the progress in developing isatin hybrids as biologically effective agents, and their crucial aspects of design and structure-activity relationships.

Design, Synthesis and Anti-Lung Cancer Evaluation of 1, 2, 3-Triazole Tethered Dihydroartemisinin-Isatin Hybrids

“…Isatin derivatives have the potential to act on a variety of drug targets like histone deacetylase, β -carbonic anhydrase, tyrosine kinase and tubulin, and the isatin-based nintedanib has already been approved for the lung cancer therapy ( Sharma et al, 2014 ; Ding et al, 2020 ; Hou et al, 2020 ; Nath et al, 2021 ; Varpe et al, 2021 ). Therefore, isatin derivatives are also considered as useful templates for the development of novel anti-lung cancer agents.…”

Schiff Base Conjugate of 5-Fluoroisatin with Thiophene-2-Ethylamine and its Mannich Bases: Synthesis, Molecular Docking, and Evaluation of in vitro Anti-inflammatory and Anti-tubercular Activity

“…[1][2][3][4] Anti-tubercular and anti-inflammatory activities of heterocyclic hybrids with isatin (indole-2,3-dione) are being studied extensively. 5,6 The Mannich bases of isatin shows potent anti-tubercular activities in previous studies. 7,8 Anti-tubercular and anti-inflammatory properties of isatin and thiophene derivatives have been reported in the literature.…”

Isatin-tethered halogen-containing acylhydrazone derivatives as monoamine oxidase inhibitor with neuroprotective effect

“…It further contains two rings: a six-membered aromatic ring and a five-membered antiaromatic ring 27 , 28 . It is widely distributed in the body fluids and different tissues of mammals and occurs naturally in plants 29 . In addition to clinical studies on the anticancer medications Toceranib, Semaxinib, and Orantinib, the Food and Drug Administration (FDA) has approved isatin-based therapies, such as Sunitinib (anti-tumor) and Nintedanib (anti-tumor) 30 – 32 (Fig.…”