Synthesis and Screening of Biologically Significant 5-Hydroxy Isatin Derivatives for Antioxidant Activity

Swathi, Konda; Sarangapani, M.

doi:10.1007/978-3-319-08927-0_14

Cited by 5 publications

(3 citation statements)

References 6 publications

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“…Antioxidant activity was reported to be associated with isatin derivatives 24,91 , N-substituted isatins 92 , 3substituted-2-oxindole derivatives 93 , 5-hydroxyisatin derivatives 94 and isatin related spiroheterocyclic compounds 95 .…”

Section: Antioxidant Activitymentioning

confidence: 99%

Review of Chemical, Pharmacological, Biological Activities of Isatin and Its Derivatives – Part-2 (2002 To 2020)

2020

JST

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: Isatin is a naturally occurring substance identified in humans, animals, plants and coal tar. Isatin derivatives are reported to possess a wide range of activites. This review is in continuation of “Part-1 (1877-2002)” review published by our team. This review encompasses the most signigicant reports published during 2002 to 2020 on the biological & pharmacological activites of isatin and its derivatives. The review includes the various synthetic reactions of isatin and activites reported. The pharmacological and biological activites reported were antimicrobial, antineoplastic & related activities; analgesic, anti-inflammatory, anticonvulsant, antioxidant, activity against veterinary pathogen, effects on cardiac & vascular smooth muscles; transthyretin fibrillogenesis inhibitor and antiglycation activity of isatin compounds.

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Section: Antioxidant Activitymentioning

confidence: 99%

Review of Chemical, Pharmacological, Biological Activities of Isatin and Its Derivatives – Part-2 (2002 To 2020)

2020

JST

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“…On the other hand, isatin is an endogenous compound identified in many organisms and possess diverse biological activities such as anti-bacterial [14], anticancer [15,16], anti-HIV [17], antimalarial [18], and anti TB activities [19], anti-oxidant [20] etc.…”

Section: Despitementioning

confidence: 99%

Synthesis, Spectral Characterization and Pharmacological Evaluation of Novel Thiazole-Oxoindole Hybrid Compounds as Potential Anticancer Agents

Ammar

El‐Sharief

Mohamed

et al. 2018

Al-Azhar Bulletin of Science

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In the present study, a series of thiazole derivatives bearing 5-morpholinosulfonylindole were designed and synthesized through condensation of 5-(morpholinosulfonyl)isatin (1) with some thiazolidinone derivatives as carbon nucleophiles to afford the corresponding arylidene derivatives (2-5, 7, 8). Furthermore, many thiazole derivatives (11-15) were obtained through the reaction of thiosemicarbazone derivative (10) with many reagents such as dimethyl acetelenedicarboxylate, phencylbromide derivatives, chloroacetonitrile, chloroacetylchloride as well as chloroacetanilide. The newly synthesized compounds were characterized based on spectral (FT-IR, 1 H NMR, 13 C NMR, MS) analysis. Cytotoxicity effects of all synthesized products were tested against three cancer cell lines, MCF-7, HepG-2, HCT-116 and they showed moderate to good cytotoxic activity against the three tested cell lines. The study showed that compounds (2a, 12b and 12c) were less or almost equipotent as doxorubicin against the three cell lines HepG-2, HCT-116.

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“…5,6 2,3-Dioxindole (isatin, I, Figure 1) is a natural substance found in some plant species, which can also be present in humans, due to endogenous consumption. Compound I has a distinguished pharmacological profile and exhibits a wide spectrum of biological actions, including anti-oxidant, 7 anti-inflammatory, 8 antibacterial, 9 and anticancer 10,11 activities. The United States Federal Drug Administration approved sunitinib and nintedanib as isatin-bearing anticancer drugs, 10,12 and many compounds with an isatin scaffold such as SU6668 and SU5416 have displayed outstanding anticancer activity.…”

Section: Introductionmentioning

confidence: 99%

<p>New Isatin–Indole Conjugates: Synthesis, Characterization, and a Plausible Mechanism of Their in vitro Antiproliferative Activity</p>

Al-Wabli

Almomen

Almutairi

et al. 2020

DDDT

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Background: Cancer remains the leading cause of human morbidity universally. Hence, we sought to assess the in vitro antiproliferative activity of new isatin-based conjugates (5a-s) against three human cancer cell lines. Methods: The antiproliferative activities of compounds 5a-s were evaluated in vitro and their ADME (absorption, distribution, metabolism and excretion) was carried out using standard protocols. Subsequently, Western blot analysis was conducted to elucidate the potential antiproliferative mechanism of compounds 5a-s. Results: The in vitro antiproliferative activities of compounds 5a-s against the tested cancer cell lines ranged from 20.3 to 95.9%. Compound 5m had an IC 50 value of 1.17 µM; thus, its antiproliferative potency was approximately seven-fold greater than that of sunitinib (IC 50 = 8.11 µM). In-depth pharmacological testing was conducted with compound 5m to gain insight into the potential antiproliferative mechanism of this class of compounds. Compound 5m caused an increase in the number of cells in the G1 phase, with a concomitant reduction of those in the G2/M and S phases. Additionally, compound 5m significantly and dose-dependently reduced the amount of phosphorylated retinoblastoma protein detected. Compound 5m enhanced expression of B cell translocation gene 1, cell cycle-associated proteins (cyclin B1, cyclin D1, and phosphorylated cyclin-dependent kinase 1), and a pro-apoptotic protein (Bcl-2-associated X protein gene), and activated caspase-3. ADME predictions exposed the oral liability of compounds 5a-s. Conclusion: Herein, we revealed the antiproliferative activity and ADME predictions of the newly-synthesized compounds 5a-s and provided a detailed insight into the pharmacological profile of compound 5m. Thus, compounds 5a-s can potentially be exploited as new antiproliferative lead compounds for cancer chemotherapeutic.

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Synthesis and Screening of Biologically Significant 5-Hydroxy Isatin Derivatives for Antioxidant Activity

Cited by 5 publications

References 6 publications

Review of Chemical, Pharmacological, Biological Activities of Isatin and Its Derivatives – Part-2 (2002 To 2020)

Review of Chemical, Pharmacological, Biological Activities of Isatin and Its Derivatives – Part-2 (2002 To 2020)

Synthesis, Spectral Characterization and Pharmacological Evaluation of Novel Thiazole-Oxoindole Hybrid Compounds as Potential Anticancer Agents

<p>New Isatin–Indole Conjugates: Synthesis, Characterization, and a Plausible Mechanism of Their in vitro Antiproliferative Activity</p>

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