Synthesis and biological evaluation of oxadiazole incorporated ellipticine derivatives as anticancer agents

Madhavi, Sapavat; Sreenivasulu, Reddymasu; Raju, Rudraraju Ramesh

doi:10.1007/s00706-016-1790-y

Cited by 49 publications

(10 citation statements)

References 32 publications

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“…Out of which, Compounds (1-4) showed higher analgesic activity. Aspirin was taken as standard drug [36][37] . Table 5.…”

Section: Anti-convulsant Activitymentioning

confidence: 99%

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2020

IJPSR

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Arylpropionic acid derivatives are an important class of NSAIDs. Ibuprofen, 2-(4-isobutylphenyl) propionic acid, is known as NSAIDs. Arylpropionic acid derivatives have a broad biological activity, including antibacterial, anticonvulsant and anticancer activity, analgesic, and anti-inflammatory. In addition to the most powerful ingredients used in analgesic and antipyretic fields, such as ibuprofen, Oxaprozin, Ketoprofen, and Phenoprofen, aryl propionic acid derivatives play an important role in treating other symptoms. The possible improvements in the activity can be further achieved by slight modifications in the substituent on the basic aryl propionic acid. According to Grigoryan et al., 2019 studies reveal that the replacement of the carboxyl group by tetrazole ring, hydroxamate, ester, alcohol, and amide groups forms compound showing lower activity (antiinflammatory, anti-nociceptive, ulcerogenic activity). The presence of a carboxyl group in the parent molecule of aryl propionic acid is important for broad-spectrum pharmacological activity. This review focused on recent advances and recent research on aryl propionic acid derivatives compared to medicinal chemistry. INTRODUCTION: Medical chemistry is an area that determines the effect of chemical composition on biological activity. Medical chemistry has been expanded with the help of experimental methods for predicting the composition of new compounds that rely heavily on structural changes and the determination of biological properties.

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“…Out of which, Compounds (1-4) showed higher analgesic activity. Aspirin was taken as standard drug [36][37] . Table 5.…”

Section: Anti-convulsant Activitymentioning

confidence: 99%

Untitled

2020

IJPSR

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“…The situation in the Latin American population is even more dramatic; according to the World Health Organization (WHO) data, 37% of cancer cases are reported in this region, and are associated with the limited development of technology and industry related to the treatment of this disease in these countries [3]. Childhood ellipticine moiety seems to have a significant influence on the compound's biological activity [36][37][38][39]. The structural similarity with ellipticine is, in theory, a fundamental key to designing new anticancer compounds.…”

Section: Introductionmentioning

confidence: 99%

Modeling the Antileukemia Activity of Ellipticine-Related Compounds: QSAR and Molecular Docking Study

et al. 2019

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The antileukemia cancer activity of organic compounds analogous to ellipticine representes a critical endpoint in the understanding of this dramatic disease. A molecular modeling simulation on a dataset of 23 compounds, all of which comply with Lipinski’s rules and have a structure analogous to ellipticine, was performed using the quantitative structure activity relationship (QSAR) technique, followed by a detailed docking study on three different proteins significantly involved in this disease (PDB IDs: SYK, PI3K and BTK). As a result, a model with only four descriptors (HOMO, softness, AC1RABAMBID, and TS1KFABMID) was found to be robust enough for prediction of the antileukemia activity of the compounds studied in this work, with an R2 of 0.899 and Q2 of 0.730. A favorable interaction between the compounds and their target proteins was found in all cases; in particular, compounds 9 and 22 showed high activity and binding free energy values of around −10 kcal/mol. Theses compounds were evaluated in detail based on their molecular structure, and some modifications are suggested herein to enhance their biological activity. In particular, compounds 22_1, 22_2, 9_1, and 9_2 are indicated as possible new, potent ellipticine derivatives to be synthesized and biologically tested.

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“…Synthesis of such heterocyclic compounds are pharmaceutical important and a foremost task of chemists due to its vast pharmacological and industrial applications. A large number of heterocyclic systems with different hetero moieties act as good anticancer agents in cancer chemotherapy and showed potent anticancer activities against a panel of human cancer cell lines [1][2][3][4][5][6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antitumor Evaluation of Novel 5-Bromo Indole-Aryl Keto Hydrazide-Hydrazone Analogues

Rudavath¹,

Sreenivasulu²,

Pinapati³

et al. 2018

Asian J. Chem.

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A wide variety of indole, substituted benzaldehyde linked keto hydrazide-hydrazone analogues were designed, synthesized and evaluated for their cytotoxicity against eight human cancer cell lines HeLa, A549, MCF-7, K562, HEK293, HT29, SF295 and HL60. All these synthesized compounds showed potent antitumor activities on the above eight human cancer cell lines. Among them, 6a and 6h compounds exhibited potent antitumor activity on HL 60 and A549 cancer cell lines with IC50 value of 3.913 and 4.838 µM than the standard drug cisplatin with IC50 values of 27 and 36 µM, respectively.

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Synthesis and biological evaluation of oxadiazole incorporated ellipticine derivatives as anticancer agents

Cited by 49 publications

References 32 publications

Untitled

Untitled

Modeling the Antileukemia Activity of Ellipticine-Related Compounds: QSAR and Molecular Docking Study

Synthesis and Antitumor Evaluation of Novel 5-Bromo Indole-Aryl Keto Hydrazide-Hydrazone Analogues

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