2016
DOI: 10.1038/srep36238
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Design, synthesis and biological evaluation of hybrids of β-carboline and salicylic acid as potential anticancer and apoptosis inducing agents

Abstract: A novel series of hybrids (7a-l, 8a-l) from β-carboline and salicylic acid (SA) were designed and synthesized, and their in vitro biological activities were evaluated. Most of the hybrids displayed potent antiproliferative activity against five cancer cell lines in vitro, showing potencies superior to 5-FU and harmine. In particular, compound 8h selectively inhibited proliferation of liver cancer SMMC-7721 cells but not normal liver LO2 cells, and displayed greater inhibitory selectivity than intermediate 5h a… Show more

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Cited by 33 publications
(12 citation statements)
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“…Many natural and synthetic agents with the ability to interact with DNA often have a relatively low therapeutic index, most likely due to the unspecific manner of these agents in causing DNA damage both in lesions and in highly proliferative normal tissues [22]. Similarly, the frequency of utilization of β-carbolines is greatly reduced because of their cytotoxic activity toward mammalian cells (low selectivity) [14,22]. We determined the cytotoxic effects of the highly bioactive quaternized derivatives 6p and 6t on BHK-21 cells (Baby hamster Syrian kidney cells).…”
Section: Resultsmentioning
confidence: 99%
“…Many natural and synthetic agents with the ability to interact with DNA often have a relatively low therapeutic index, most likely due to the unspecific manner of these agents in causing DNA damage both in lesions and in highly proliferative normal tissues [22]. Similarly, the frequency of utilization of β-carbolines is greatly reduced because of their cytotoxic activity toward mammalian cells (low selectivity) [14,22]. We determined the cytotoxic effects of the highly bioactive quaternized derivatives 6p and 6t on BHK-21 cells (Baby hamster Syrian kidney cells).…”
Section: Resultsmentioning
confidence: 99%
“…HBL-100 cells were sensitive to m-fluoro phenyl-1,2,3-triazolyl harmine and the IC 50 value was 16 μM, less than 32 μM of harmine [ 34 ]. A series of novel harmine derivatives transformed at 1 and 3 substitutes were synthesized and their cytotoxicity against human cancer cell lines were detected by MTT; some potential compounds exhibited higher inhibition activities than harmine [ 35 , 36 ]. The 2-thioxo-1,3,4-oxadiazole derivatives with special biological activities have attracted more and more attention and have been widely used in drug and pesticide molecular design in recent years [ 37 , 38 , 39 , 40 ].…”
Section: Discussionmentioning
confidence: 99%
“…Additionally, B-9-3 elevated apoptotic rate by disrupting VEGF-A/VEGFR2 pathway (Ma et al, 2016). A hybrid of hydroxamic acid and β-carboline alkaloid harmine exhibited cytotoxicity against lung carcinoma (H460) cells through apoptosis induction associated with the activation of Bax, and down-regulating the Bcl-2 expression (Xu et al, 2016), and also known to have protective effects against A549 cancer cells (Filali et al, 2015;Du et al, 2016).…”
Section: Anti-cancer Activitymentioning
confidence: 99%
“…Harmine and its derivatives have been investigated for their anti-cancer activities against colon HCT-116 cells (Filali et al, 2015;Filali et al, 2016;Xu et al, 2016;Zhang et al, 2016) (Figure 3). In another study, harmine exhibited anti-proliferative effect against colon (Caco2) cancer cells through inhibition of protein kinase DYRK1A (Bruel et al, 2014).…”
Section: Anti-cancer Activitymentioning
confidence: 99%
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