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001-es BibID:	BIBFORM086917
Első szerző:	Borazjani, Nassim
Cím:	Cytotoxicity, anticancer, and antioxidant properties of mono and bis-naphthalimido β-lactam conjugates / Nassim Borazjani, Maryam Behzadi, Marzieh Dadkhah Aseman, Aliasghar Jarrahpour, Javad Ameri Rad, Sedigheh Kianpour, Aida Iraji, S. Masoud Nabavizadeh, Mohammad Mehdi Ghanbari, Gyula Batta, Edward Turos
Dátum:	2020
ISSN:	1054-2523
Megjegyzések:	This article reports the diastereoselective synthesis of some novel naphthalimido and bis-naphthalimido beta-lactam derivatives and a preliminary evaluation of their anticancer properties. The reactions were completely diastereoselective, leading exclusively to the formation of cis-beta-lactams 11a-l and trans-bis-beta-lactams 16a-g. All of these compounds were obtained in good to excellent yields and their structures were established based on IR, H-1 NMR, C-13 NMR spectral data, and elemental analysis. Each of the beta-lactams was screened for antioxidant and anticancer activities. Our results showed that all the compounds lacked cytotoxicity against HepG2 cells, whereas 16a and 16b exhibited excellent anticancer activity with IC50 values below 191.57 mu M on MCF-7 cell line and also, bis-beta-lactams 16a-g showed excellent antitumor activity against the TC-1 cell line. Antioxidant experiments of 16a-d by the diphenylpicrylhydrazyl (DPPH) assay showed IC50 values ranging from 7 to 32.3 mu g/ml. Interaction of 16a, 16b, 16d-g with calf-thymus DNA (CT-DNA) was also supported by absorption titration studies. The compounds exhibit good binding propensity to CT-DNA and the DNA binding affinity (K-b) of the compounds varies as 16a; 16b; 16e; 16g > 16d; 16f. Interaction of 16d with CT-DNA was also investigated by fluorescence spectroscopy. The results support an intercalative interaction of 16d and 16f and non-intercalation mechanism for 16a, 16b, 16e, and 16g.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Anticancer Antioxidant Cytotoxicity Diastereoselective β-lactam
Megjelenés:	Medicinal Chemistry Research. - 29 : 8 (2020), p. 1355-1375. -
További szerzők:	Behzadi, Maryam Dadkhah Aseman, Marzieh Jarrahpour, Aliasghar Rad, Javad Ameri Kianpour, Sedigheh Iraji, Aida Nabavizadeh, S. Masoud 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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