Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents

Kamal, Ähmed; Bharathi, E. Vijaya; Reddy, Jhansi; Ramaiah, M. Janaki; Dastagiri, D.; Reddy, M. Kashi; Arutla, Viswanath; Teegala, Lakshminarayan Reddy; Shaik, Thokhir Basha; Pushpavalli, S. N. C. V. L.; Bhadra, Manika Pal

doi:10.1016/j.ejmech.2010.12.004

Cited by 154 publications

(51 citation statements)

References 26 publications

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“…Some 2-spirooxindole dihydroquinazolinones demonstrate anti-bacterial activity in vitro. 8 Several methods have been reported for the preparation of 2-substituted 2,3-dihydroquinazolin-4(1H)-ones, based mainly on the cyclocondensation of anthranil(onitrile)amides with aldehydes in the presence of various catalysts such as cyanuric chloride, 9 citric acid 10 , ZnCl2, 11 p-TSA 12 and sulfamic acid 13 . Moreover, many of these protocols are associated with the application of exotic catalyst systems, extended reaction times and tedious work-up procedures.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 2-(hetero)arylquinazolinones in aqueous media

Tmea¹,

Mikls²,

Lzr³

et al. 2017

Arkivoc

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Mechanochemical treatment of N-unsubstituted or N-methyl anthranilamide with benzaldehyde yielded their Schiff bases derivatives which could be easily cyclized to the corresponding 2-phenyl-2,3-dihydroquinazolinones via thermal rearrangement in water. On the basis of the above findings, an eco-friendly method was applied to prepare quinazolin-4(1H)-one derivatives from anthranilamides and a number of (hetero)aryl aldehydes. Heating the aqueous mixture of starting compounds to 90 °C resulted in the products in 81-94% yields. All products precipitated from the reaction mixture and were isolated by simply filtration. No further work-up or purification was necessary.

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Section: Introductionmentioning

confidence: 99%

Synthesis of 2-(hetero)arylquinazolinones in aqueous media

Tmea¹,

Mikls²,

Lzr³

et al. 2017

Arkivoc

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“…20 The number of viable cells was found to be proportional to the extent of formazan production by the cells used. These tests, which depend on the ability of cells to survive a toxic insult, were carried out by using 96-well microtitre plates.…”

Section: Assessment Of Cytotoxicity By Mtt Assaymentioning

confidence: 99%

Utility of Isatin Semicarbazones in Mammary Carcinoma Cells - A Proof of Concept Study

Sathianarayanan¹,

Chittethu²,

Jose³

et al. 2017

JYP

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Objective: The present study was aimed to determine cytotoxic and apoptotic activity of isatin semicarbazones against mammary carcinoma. Methodology: The preparation of these target compounds involved substitution at the third position of the isatin nucleus along with chemical modification at the nitrogen atom of the scaffold to obtain more potent derivatives. The synthesized analogs were characterized by recording their melting point and R f values along with IR, NMR and mass spectra. An antioxidant study and Cytotoxic Studies were performed by DPPH, Nitric oxide scavenging method and MTT assay methods. Results: The results revealed that all the test compounds (5a-5d) exhibited good anti oxidant activity. The synthesized compounds were then screened for in-vitro cytotoxicity by MTT cell proliferation assay method against breast cancer cell lines including MCF-7 and BT-549 with derivative 5a exhibiting maximum activity in both the cell lines. DNA fragmentation studies further indicated that 5a was involved in apoptotic process. Conclusion: Interestingly, it was observed that while all the synthesized compounds seemed active, 5a exhibited a superior ability to induce apoptosis.

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“…2,3-Dihydroquinazolinones represent a family of drugs that are used as anticancer, antibiotic, anti-inflammatory, analgesic, diuretic, antidepressant, and antitubercular behaviour [5][6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%