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001-es BibID:	BIBFORM084070
Első szerző:	Borazjani, Nassim
Cím:	Three-component synthesis of chromeno β-lactam hybrids for inflammation and cancer screening / Nassim Borazjani, Saghi Sepehri, Maryam Behzadi, Aliasghar Jarrahpour, Javad Ameri Rad, Maryam Sasanipour, Milad Mohkam, Younes Ghasemi, Amin Reza Akbarizadeh, Carole Digiorgio, Jean Michel Brunel, Mohammad Mehdi Ghanbari, Gyula Batta, Edward Turos
Dátum:	2019
ISSN:	0223-5234
Megjegyzések:	Highly diastereoselective synthesis of chromeno b-lactam hybrids was achieved by an efficient one-pot three-component reaction. With this procedure, the desired b-lactam products were obtained in good yields and with exclusive cis stereoselection, by combining a variety of benzaldehydes, malononitrile, and either 5,5-dimethylcyclohexane-1,3-dione or 4-hydroxycoumarin in the presence of 1,4-diazabicyclo [2.2.2]octane under reflux conditions. These adducts were structurally characterized on the basis of IR, 1D and 2D NMR spectra, X-ray analysis, HeH COSY and HeC HSQC two-dimensional NMR experiments, and elemental analysis. Each of the synthesized compounds was screened for anti-inflammatory and anticancer activities. b-Lactams 5b and 8b showed a 53.4 and 19.8 anti-inflammatory ratio, respectively, and 5b appeared more active than the well-known dexamethasone corticosteroid used for the treatment of rheumatoid and skin inflammation. b-Lactams 5a, 5b, 5e, 5f, 5g, 8c, 8j and 8p also showed good antitumor activity against the SW1116 (colon cancer) cell line without notable cytotoxicity towards the HepG2 control cell line.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Anticancer Anti-inflammatory β-lactam Colon cancer Cytotoxicity DABCO
Megjelenés:	European Journal of Medicinal Chemistry. - 179 (2019), p. 389-403. -
További szerzők:	Sepehri, Saghi Behzadi, Maryam Jarrahpour, Aliasghar Rad, Javad Ameri Sasanipour, Maryam Mohkam, Milad Ghasemi, Younes Akbarizadeh, Amin Reza Digiorgio, Carole Brunel, Jean Michel Ghanbari, Mohammad M. Batta Gyula (1953-) (molekula-szerkezet kutató) Turos, Edward
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001-es BibID:	BIBFORM078606
Első szerző:	Borazjani, Nassim
Cím:	Design, synthesis and biological evaluation of some novel diastereoselective β-lactams bearing 2-mercaptobenzothiazole and benzoquinoline / Nassim Borazjani, Aliasghar Jarrahpour, Javad Ameri Rad, Milad Mohkam, Maryam Behzadi, Younes Ghasemi, Somayyeh Mirzaeinia, Hamid Reza Karbalaei-Heidari, Mohammad Mehdi Ghanbari, Gyula Batta, Edward Turos
Dátum:	2019
ISSN:	1054-2523
Megjegyzések:	We report the synthesis of some novel β-lactam hybrids of 2-mercaptobenzothiazole and benzoquinoline. These compounds were synthesized by a [2 + 2]-cycloaddition reaction of imines 8a-d and ketenes derived from substituted acetic acids. The reaction was totally diastereoselective leading exclusively to the formation of cis-β-lactams 10a-m. All products were obtained in good to excellent yields and their structures were established based on IR, 1H NMR, 13C NMR spectral data and elemental analysis. Schiff bases 8a-d and β-lactam hybrids 10a-m were evaluated for antimicrobial activities against six bacterial species. The minimum inhibitory concentration (MIC) values indicate that two of the β-lactams, 10k and 10m, have good activities against the two Gram-negative bacteria, E. coli and P. aeruginosa, while three of the Schiff bases, 8a-c, are active against P. aeruginosa and the Gram-positive pathogen S. aureus. The molecular and cellular basis for these observed antibacterial properties are not determined. Moreover, the five most active compounds showed acceptably low cytotoxicity (less than 25% cell growth inhibition after 72 h of incubation) against the MCF-7 cell line, and below 10% in vitro hemolytic activity at 50 and 200 ?M concentrations. These results suggest a need for further inquiry into the reason for why these compounds are bioactive, and as to what their full biological activities and antibiotic potential may be. The cis stereochemistry of β-lactam 10a was confirmed by X-ray crystallographic studies.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban β-Lactam Hybrid 2-Mercaptobenzothiazole Benzoquinoline Antimicrobial Hemolysis Mammalian cell toxicity
Megjelenés:	Medicinal Chemistry Research. - 28 : 3 (2019), p. 329-339. -
További szerzők:	Jarrahpour, Aliasghar Rad, Javad Ameri Mohkam, Milad Behzadi, Maryam Ghasemi, Younes Mirzaeinia, Somayyeh Karbalaei-Heidari, Hamid Reza Ghanbari, Mohammad M. Batta Gyula (1953-) (molekula-szerkezet kutató) Turos, Edward
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
Borító:
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