Abstract
The results of our previous research indicated that some derivatives of benzofurans, particularly halogeno-derivatives, are selectively toxic towards human leukemia cells. Continuing our work with this group of compounds we here report new data on the synthesis as well as regarding the physico-chemical and biological characterization of fourteen new derivatives of benzofurans, including six brominated compounds. The structures of all new compounds were established by spectroscopic methods (1H- and, 13C-NMR, ESI MS), and elemental analyses. Their cytotoxicity was evaluated against K562 (leukemia), MOLT-4 (leukemia), HeLa (cervix carcinoma), and normal cells (HUVEC). Five compounds (1c, 1e, 2d, 3a, 3d) showed significant cytotoxic activity against all tested cell lines and selectivity for cancer cell lines. The SAR analysis (structure-activity relationship analysis) indicated that the presence of bromine introduced to a methyl or acetyl group that was attached to the benzofuran system increased their cytotoxicity both in normal and cancer cells.
Highlights
All of the new benzofuran derivatives related to X are characterized by lower clogP values when compared to the lead compound, indicating their improved solubility in aqueous media (Table 1)
We have identified five compounds 1c, 1e, 2d, 3a, and 3d in the initial screening, which, at the concentration of 100 μM, reduced the viability of all tested cancer cells K562, HeLa and MOLT-4
Compound 1e shows the cytotoxic property, and contains an acetyl halide substituent in the benzene ring and a bromine atom that is directly attached to the furan ring
Summary
Ienntzroofduurcatniosnkeleton holds an important position in organic chemistry and it is considered to be oneBeonfztohfeurmanosskt eimletpoonrthaonltdshaenteirmocpyocrlitcanstypstoesmitisonbeincaoursgeanoifcictshedmivisetrrsye apnrdofiitleis ocfonbsioidloergeidcatlo be activointye. AndTshyinsthstertuicctbuernalzoufnuirtains daercievnattriavleps ahratvoef baeevnarrieeptyorotef dbitoolopgoiscsaellsys awcitdiveethcoemrappoeuutnidc sp. Ias, and by BNufouwraalodla, yws,hwichheins caanncoenr-,sapfetceirficcaβrd-aiodvreansceurglaicr dbilsoecakseers,wisiththaenseacfofinnditymfoosrt βco1mamndonβ2c-aaudsreenoefrgic deatrhecaenpdtosrtsil[l3c,o4n,7s]t.itutes an unresolved problem of clinical medicine and pharmacology, extensive research regarding new anticancer compounds is especially important. These new drugs should possess improved pharmacokinetics and destroy cancer cells, without causing negative. Research in the group of benzofuran derivatives is justified, especially by the fact that one can find many examples of data in the literature on benzofurans with anticancer activity. In many cases,Mtohleecublees n20z1o9,f2u4r, xan skeleton is fused with other heterocyclic or aromatic moieties (Figure22o)f.17
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