Syntheses of heterocyclic derivatives as potential cytotoxic compounds evaluated toward hepatocellular and cervical carcinoma cell lines

Mohareb, Rafat M.; Ibrahim, Bishoy A.

doi:10.4314/bcse.v37i1.12

Cited by 2 publications

(3 citation statements)

References 27 publications

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“…Considering the pyran derivatives 5a-m, where the data in Table 1 demonstrated that compounds 5a, 5c, 5d, 5e, 5f, 5g, 5h and 5i were the most cytotoxic compounds among these compounds. Table 1 showed that compounds 5e (X = Cl, R = R'= CN), 5f (X = Cl, R = COOEt, R' = CN) and 5g (X = Cl, R = CN, R' = COOEt) exhibited higher inhibitions than the reference 0.08 ± 0.01 0.18 ± 0.03 0.15 ± 0.023 0.03±0.0055 0.90 ± 0.13 0.44 ± 0.062 a IC50's of Foretinib against cancer cell lines was taken identical to the previously reported work [32][33][34].…”

Section: Sar's (Structure Activity Relationship) Of the Synthesized C...mentioning

confidence: 53%

“…The variations of substituents within the ring system beside the nature of the heterocyclic compound had a notable impact on the anti-proliferative activity. Through such measurements the IC50's of Foretinib demonstrated in Table 1 against the cancer cell lines were considered identical to the previously reported work [32][33][34].…”

Section: Biology Anticancer Evaluations Of the Newly Synthesized Comp...mentioning

confidence: 58%

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Anti-proliferative activities of 4H-pyran derivatives synthesized from benzoylacetone

Mohareb¹,

Ibrahim²,

Farouk³

2022

Bull. Chem. Soc. Eth.

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ABSTRACT. Benzoylacetone (1) underwent a series of multi-component reactions with aromatic aldehydes and malononitrile or ethyl cyanoacetate to produce the pyran derivatives 4a-f. The latter compounds reacted with malononitrile or ethyl cyanoacetate to yield the condensation products 5a-m. On the other hand, the reaction of 4a-f with either the diazonium salts 6a-c yielded the arylhydrazone derivatives 7a-i. The multi-component reaction of (1) with aromatic adehydes and cyclohexan-1,3-dione produced the pyran derivatives 9a-c. Compound 1 underwent the Gewald’s reactions with elemental sulfur and malononitrile or ethyl cyanacetate yielding the thiophene derivatives 10a,b. Evaluations of the synthesized products were carried out against some selected cancer cell lines and the most active compounds were further evaluated against the seventeen cancer cell lines classified according to the disease. Morphological changes of A549 cell line by the effect of compound 7k was studied using microenvironment of the lung tissue where an excellent results was obtained. KEY WORDS: Benzoylacetone, Multi-component reactions, Pyran, Thiophene, Arylhydrazone, Cytotoxicity Bull. Chem. Soc. Ethiop. 2023, 37(2), 405-425. DOI: https://dx.doi.org/10.4314/bcse.v37i2.12

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Section: Sar's (Structure Activity Relationship) Of the Synthesized C...mentioning

confidence: 53%

Section: Biology Anticancer Evaluations Of the Newly Synthesized Comp...mentioning

confidence: 58%

Anti-proliferative activities of 4H-pyran derivatives synthesized from benzoylacetone

Mohareb¹,

Ibrahim²,

Farouk³

2022

Bull. Chem. Soc. Eth.

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“…Recently, our research group was concerned with different multi-component reactions aiming to produce new heterocyclic compounds characterized by different substituents. This enhanced us to study plenty of structure activity relationship and thus producing new cytotoxic agents [26][27][28][29][30]. The pyrazole derivatives 1a-f were synthesized, where such compounds were used as the key starting compounds for the synthesis of new heterocyclic compounds.…”

Section: Resultsmentioning

confidence: 99%

Multi-component synthesis of pyrazolo[1,5-a]quinazoline, thiazole and thiophene derivatives as cytotoxic agents

Mohareb,

E. Helal,

Mayhoub

et al. 2023

Bull. Chem. Soc. Eth.

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ABSTRACT. This study demonstrated the synthesis of a number of pyrazolo[1,5-a]quinazoline derivatives about 24 products based on the starting material 4-(2-phenylhydrazono)-4H-pyrazol-3-amine derivatives 1a-f. Moreover, other ring systems including thiophene, pyrazole, thiazole and pyran (16 compounds) were prepared based on another starting compounds 2-(furan-2-ylmethylene)cyclohexane-1,3-dione 10 and 5,5-dimethyl-3-phenyl-2-thioxo-2,3,5,6-tetrahydrobenzo[d]thiazol-7(4H)-one 18. The multi-component reaction was used to prepare all the previous compounds. The structures of all the synthesised compounds were confirmed by the analytical and spectral data. Some selected compounds were chosen to test their anticancer activity against six cancer cell lines, namely A549, HT-29, MKN-45, U87MG, SMMC-7721 and, H460 utilizing foretinib as the positive control and the standard MTT assay in vitro. Toward the tested cell lines, nine compounds were the most cytotoxic compounds. The results obtained revealed that the synthesized compounds are good cytotoxic agents and of great impact for future work. KEY WORDS: Multi-component reactions, Pyrazolo[1,5-a]quinazoline, Thiophene, Thiazole, Cytotoxicity Bull. Chem. Soc. Ethiop. 2023, 37(6), 1521-1538. DOI: https://dx.doi.org/10.4314/bcse.v37i6.17

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Syntheses of heterocyclic derivatives as potential cytotoxic compounds evaluated toward hepatocellular and cervical carcinoma cell lines

Cited by 2 publications

References 27 publications

Anti-proliferative activities of 4H-pyran derivatives synthesized from benzoylacetone

Anti-proliferative activities of 4H-pyran derivatives synthesized from benzoylacetone

Multi-component synthesis of pyrazolo[1,5-a]quinazoline, thiazole and thiophene derivatives as cytotoxic agents

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