Abstract
Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.
Highlights
Heterocyclic entities are denoted as a vital class of organic compounds with wide biological and pharmacological potency [1,2]
The results showed that many synthesized hybrids have potent activity against M. tuberculosis (MTB) H37Ra
The obtained results revealed that compounds 53b, 53c, 53h, and 53i displayed promising antimicrobial potential with MIC 7.81 mg/mL which is better than the reference ciprofloxacin against S. aureus and S. epidermidis
Summary
Heterocyclic entities are denoted as a vital class of organic compounds with wide biological and pharmacological potency [1,2]. The molecular hybrids were assessed for their anticancer potency against eight human cancer cell lines, namely, HepG2, Hela, HCT-116, A549, DU145, SKOV3, MCF-7, and MCF-7/DOX (Doxorubicin-resistant MCF-7) via SRB assay using etoposide as the positive control It was suggested by the research group that eight bis-isatin analogues exhibited excellent potency against all screened human cancer cell lines with IC50 values between 8.32 and 49.73 μM. SAR analysis displayed that bis-isatin analogues substituted at C-3 and C-5 positions of isatins could exhibit potential anticancer activity against tested human cancer cell lines. Furnished hybrids were screened for their anticancer potency against A549, HepG2, MCF-7, PC-3, and HeLa human cancer cell lines using a CCK-8 Assay Kit. The majority of the analogues were found active against tested cell lines, amidst compounds 14g and 14h with IC50 values of 77.2–88.9 μM and 65.4–89.7 μM, respectively. Semicarbazones, and hydrazone oximes could boost the potency
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