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 in discovering 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 for designing new molecules based on isatin nucleus analysis of various
pharmacophore hybrids, spacers/linkers between pharmacophores and isatin for hybridization and
their biological activities are important. This review discusses the progress in developing isatin hybrids
as biologically effective agents and their crucial aspects of design and structure-activity relationships.
Keywords: Hybridization, Molecular hybrids, anticancer, anti-HIV, antimalarial, antitubercular, antibacterial.
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