ChemInform Abstract: Synthesis, Characterization and Cytotoxic Activity of New Salicylaldehyde Benzoylhydrazone Derivatives as Potential Antiproliferative Agents.

Nikolova-Mladenova, Boryana; Halachev, Nenko; Iankova, Rumjana; Momekov, Georgi; Ivanov, D.

doi:10.1002/chin.201216214

Cited by 1 publication

(5 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The findings presented here are a continuation of our previous research on salicylaldehyde hydrazones with anticancer activity [ 26 , 27 , 28 , 29 , 30 , 31 , 32 ]. A set of eleven compounds synthesized and tested before was used as a training set and SAR analyses were performed for cytotoxic activity on HL-60, KE-37, K-562, BV-173, SaOS-2, and MCF-7 cell lines.…”

Section: Discussionsupporting

confidence: 84%

“…In the present study, we consider the anticancer activity of the compounds on seven cell lines (HL-60, KE-37, K-562, BV-173, SaOS-2, MDA-MB-231, and MCF-7) and express it as IC 50 values. Some of the activities have been published before [ 26 , 27 , 28 , 29 , 30 , 31 , 32 ], the rest were measured for the aim of the present study. The cell lines HL-60, KE-37, K-562, and BV-173 are isolated from patients with different types of leukemia: acute promyelocytic leukemia (HL-60), acute lymphoblastic leukemia (ACC) (KE-37), and chronic myeloid leukemia (K-562 and BV-173), while SaOS-2 cells originate from human osteosarcoma.…”

Section: Resultsmentioning

confidence: 99%

“…The 4-methoxysalicylaldehyde-based hydrazones were synthesized by the reaction of Schiff base condensation in ethanol, as previously described [ 26 , 27 , 28 , 29 ] according to Scheme 1 . The hydrazones were obtained in high yields and their structures were identified using a variety of analytical and spectroscopic techniques.…”

Section: Resultsmentioning

confidence: 99%

“…The training set of salicylaldehyde hydrazones contained 11 compounds synthesized and tested before in our Lab [ 26 , 27 , 28 , 29 , 30 , 31 , 32 ]. Their anticancer activities were measured and expressed as IC 50 values on the following cell lines: HL-60, KE-37, K-562, BV-173, SaOS-2, MDA-MB-231, and MCF-7.…”

Section: Methodsmentioning

confidence: 99%

“…The investigations demonstrated that the presence of methoxy group in salicylaldehyde results in derivatives with high antiproliferative activity. 3-methoxysalicylaldehyde-derived hydrazones cause strong cytotoxic effects against the leukemic cell lines, especially those of AML HL-60 cells [ 26 , 27 ]. The presence of a methoxy group in the 5th position in salicylaldehyde hydrazones causes remarkable activity against the solid breast cancer cell line MCF-7 with IC 50 values of 0.91–3.54 μmol/L [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

See 4 more Smart Citations

Design, Synthesis and Cytotoxic Activity of Novel Salicylaldehyde Hydrazones against Leukemia and Breast Cancer

Nikolova-Mladenova

Momekov

Zhivkova

et al. 2023

IJMS

View full text Add to dashboard Cite

Despite the significant advancements in complex anticancer therapy, the search for new and more efficient specific anticancer agents remains a top priority in the field of drug discovery and development. Here, based on the structure-activity relationships (SARs) of eleven salicylaldehyde hydrazones with anticancer activities, we designed three novel derivatives. The compounds were tested in silico for drug-likeness, synthesized, and evaluated in vitro for anticancer activity and selectivity on four leukemic cell lines (HL-60, KE-37, K-562, and BV-173), one osteosarcomic cell line (SaOS-2), two breast adenocarcinomic cell lines (MCF-7 and MDA-MB-231), and one healthy cell line (HEK-293). The designed compounds were found to have appropriate drug likeness and showed anticancer activities in all cell lines tested; particularly, two of them exhibited remarkable anticancer activity in nanomolar concentrations on the leukemic cell lines HL-60 and K-562 and the breast cancer MCF-7 cells and extraordinary selectivity for the same cancer lines ranging between 164- and 1254-fold. The study also examined the effects of different substituents on the hydrazone scaffold and found that the 4-methoxy salicylic moiety, phenyl, and pyridinyl rings are the most appropriate for anticancer activity and selectivity of this chemical class.

show abstract