Evaluation of the Anticancer Activities of Isatin-Based Derivatives

Gideon, Daniel Andrew; Annadurai, Pushparaj; Nirusimhan, Vijay; Parashar, Abhinav; James, Joel; Dhayabaran, V. Violet

doi:10.1007/978-981-16-1247-3_51-1

Cited by 3 publications

(3 citation statements)

References 66 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Several compounds of the tested series displayed significant anti-cancer activity, particularly compounds 5a, 5b, 5c and 5d displayed IC50 below 10 µM against the tested cell lines [40]. Structural analog of isatin, specially oxindole moiety recognized as privileged for anti-cancer drug discovery, afforded several approved drug candidates as well as lead compounds [41][42][43]. Naggar et al [44] designed and synthesized two series of compounds based upon thiazolidinone-isatin and thiazolo-[3,2-a]-benzimidazolone-isatin.…”

Section: Tri-substituted Thiazolidine-4-one Derivatives As Anti-cance...mentioning

confidence: 99%

Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Singh¹,

Piplani²,

Kharkwal³

et al. 2023

Pharmacophore

View full text Add to dashboard Cite

show abstract

Section: Tri-substituted Thiazolidine-4-one Derivatives As Anti-cance...mentioning

confidence: 99%

Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Singh¹,

Piplani²,

Kharkwal³

et al. 2023

Pharmacophore

View full text Add to dashboard Cite

show abstract

Section: Introductionmentioning

confidence: 99%

“…[32] Spirooxindole derivatives have greater target specificity and lower toxicity against noncancerous cells and have been demonstrated to have potent anticancer activities in several models of human cancer cell lines. [65] In this study, the newly synthesized pyrazole-engrafted spiro molecules were evaluated for their potential ability to inhibit the proliferation of the liver cancer cell line HepG2 and the MCF-7 breast cancer cell line. Compounds with promising antiproliferative activity were assessed for their potential dual EGFR/CDK-2 inhibitory activity, progression, and cell apoptosis.…”

mentioning

confidence: 99%

Synthesis and SARs study of novel spiro‐oxindoles as potent antiproliferative agents with CDK‐2 inhibitory activities

Al‐Jassas,

Islam,

Al‐Majid

et al. 2023

Archiv der Pharmazie

View full text Add to dashboard Cite

A series of 16 novel spirooxindole analogs 8a-p were designed and constructed via cost-effective single-step multicomponent [3+2] cycloaddition reaction of azomethine ylide (AY) generated in situ from substituted isatin (6a-d) with suitable amino acids (7a-c) and ethylene-engrafted pyrazole derivatives (5a,b). The potency of all compounds was assayed against a human breast cancer cell line (MCF-7) and a human liver cell line (HepG2). Spiro compound 8c was the most active member among the synthesized candidates, with exceptional cytotoxicity against the MCF-7 and HepG2 cell lines, with IC 50 values of 0.189 ± 0.01 and 1.04 ± 0.21 µM, respectively. The candidate 8c exhibited more potent activity (10.10-and 2.27-fold) than the standard drug roscovitine (IC 50 = 1.91 ± 0.17 µM (MCF-7) and 2.36 ± 0.21 µM (HepG2)). Compound 8c was investigated for epidermal growth factor receptor (EGFR) inhibition; it exhibited promising IC 50 values of 96.6 nM compared with 67.3 nM for erlotinib. The IC 50 value of 8c (34.98 nM) exhibited cyclin-dependent kinase 2 (CDK-2) inhibition, being more active than roscovitine the (IC 50 = 140 nM) in targeting the CDK-2 kinase enzyme.Additionally, for apoptosis induction of compound 8c in MCF-7, it upregulated the expression levels of proapoptotic genes for P53, Bax,8, and 9 at up to 6.18, 4.8, 9.8, 4.6,11.3 fold-change, respectively, and downregualted the level of the antiapoptotic gene for Bcl-2 by 0.14-fold. Finally, a molecular docking study of the most active compound 8c highlighted a good binding affinity with Lys89 as the key amino acid for CDK-2 inhibition.

show abstract

Synthesis and SAR of morpholine and its derivatives: A review update

Jain,

Kumar Sahu

2024

E3S Web Conf.

View full text Add to dashboard Cite

Morpholine is a stretchy moiety, a special pharmacophore and an amazing heterocyclic compound with wide scopes of pharmacological exercises because of various pharmacological of activity. The capacity of morpholine to upgrade the power of the particle through sub-atomic collaborations with the objective protein (kinases) or to modify the pharmacokinetic properties impelled restorative scientific experts and specialists to orchestrate morpholine ring by the proficient ways and to fuse this moiety to create different lead compound with assorted therapeutic activity. Morpholine is an organic substance compound having a six-membered ring containing two heteroatom nitrogen(N) and oxygen(O), considered as the significant core in restorative and medicinal chemistry. The current study essentially centered around talking about the most encouraging synthesis leads containing compound morpholine ring alongside structure-activity relationship (SAR) to uncover the dynamic pharmacophores responsible for anticancer, mitigating, antiviral, anticonvulsant, antihyperlipidemic, cell reinforcement, antimicrobial and antileishmanial action. This audit will give the essential information base to the medicinal chemistry in rolling out vital basic improvements in structuring morpholine subsidiaries.

show abstract

Evaluation of the Anticancer Activities of Isatin-Based Derivatives

Cited by 3 publications

References 66 publications

Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review

Synthesis and SARs study of novel spiro‐oxindoles as potent antiproliferative agents with CDK‐2 inhibitory activities

Synthesis and SAR of morpholine and its derivatives: A review update

Contact Info

Product

Resources

About