1186385-96-5Relevant academic research and scientific papers
Cytotoxicity, anticancer, and antioxidant properties of mono and bis-naphthalimido β-lactam conjugates
Borazjani, Nassim,Behzadi, Maryam,Dadkhah Aseman, Marzieh,Jarrahpour, Aliasghar,Rad, Javad Ameri,Kianpour, Sedigheh,Iraji, Aida,Nabavizadeh, S. Masoud,Ghanbari, Mohammad Mehdi,Batta, Gyula,Turos, Edward
, p. 1355 - 1375 (2020)
This article reports the diastereoselective synthesis of some novel naphthalimido and bis-naphthalimido β-lactam derivatives and a preliminary evaluation of their anticancer properties. The reactions were completely diastereoselective, leading exclusively to the formation of cis-β-lactams 11a–l and trans-bis-β-lactams 16a–g. All of these compounds were obtained in good to excellent yields and their structures were established based on IR, 1H NMR, 13C NMR spectral data, and elemental analysis. Each of the β-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 μM on MCF-7 cell line and also, bis-β-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 μg/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 (Kb) 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.
Hybrid pharmacophore design and synthesis of naphthalimide-benzimidazole conjugates as potential anticancer agents
Kamal, Ahmed,Kumar, Pogula Praveen,Khan, Mohammed Naseer Ahmed,Sheshadri, Bobburi Naga,Srinivas, Olepu
, p. 374 - 384 (2015/06/22)
Naphthalimide-benzimidazole conjugates were prepared using two different types of spacer units; either a simple alkane chain or a substituted piperazine moiety with variable alkyl side chains. Each set of conjugates was evaluated for their in vitro antica
NOVEL NAPTHALIMIDE-BENZIMIDAZOLE HYBRIDS AS POTENTIAL ANTITUMOUR AGENTS AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 10, (2009/10/22)
The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of gene
