KB Cell Lines Research Articles

Kinetics of cell death triggered photothermally using folate-conjugated gold nanoparticles and various laser irradiation conditions in cancer cells

Introduction: In this study, we explore in detail cell-specific targeting efficacy of nano-photo-thermal therapy (NPTT) method and the resulting responses that are induced by variable laser intensities and exposure times in cancer cells to induce selective apoptosis. We delineate the synthesis of a high-yielding synthetic F-AuNPs by tailoring the surface of gold nanoparticles with folic acid to enhance cell selectivity and specificity. Materials and Methods: For this purpose, synthesized F-AuNPs treated cells were irradiated with various laser intensities and exposure duration. Both KB cancer cells, as a folate receptor over-expressing cell line, and L929 normal cells, with low level of folate receptors were used. Following various regimes of NPTT, Cytotoxicity was assessed by MTT assay and comparison of induced apoptosis and necrosis in population of cells were depicted by Annexin/PI staining. Results: We report no significant cytotoxicity difference between KB and L929 cell lines at concentrations up to 40 μM of F-AuNPs. Moreover, no significant cell lethality occurred for various laser irradiation conditions. However, in photothermal therapy, the viability of KB and L929 cells was 57% and 83%, respectively. Flow cytometry clearly revealed the kinetics of cell death. The majority of cancer cell death was related to apoptosis (41% apoptosis of 43% overall cell death). Conclusion: Together, these findings confirm that F-AuNPs based NPTT can either induces cell death via apoptosis or necrosis. The main factor determining whether a cell will die due to apoptosis or necrosis on-demand with PTT depends on laser heating level. Our main target must be to only trigger apoptosis during PTT by using suitable irradiation conditions. As a result, folate targeting ability of the F-AuNPs and laser energy threshold to induce selective apoptosis in cancer cells were shown.

Design, Synthesis and Cytotoxic Evaluation of 4-Anilinoquinazoline– triazole–AZT Hybrids as Anticancer Agents

A series of 4-anilinoquinazoline–triazole–AZT hybrids were designed and synthesized as anticancer agents. Their cytotoxic potential has been evaluated by means of a micro-dilution assay against three human cancer cell lines (KB, epidermoid carcinoma; HepG2, hepatoma carcinoma; SK-Lu-1, non-small lung cancer). The biological results revealed that compounds 4b and 6d showed good anticancer activities against KB, HepG2, and Lu cell lines (IC50 values ranging from 9 μM to 100 μM). Especially, compounds 4b and 6d exhibited up to 3-fold more potent than reference drugs erlotinib hydrochloride and AZT in term of anti-lung cancer activity.

Cytotoxic and apoptotic potential of Myristica fragrans Houtt. (mace) extract on human oral epidermal carcinoma KB cell lines

Several studies have revealed that certain naturally occurring medicinal plants inhibit the growth of various cancers. The present study was conducted to evaluate cytotoxicity and apoptotic induction potential of Myristica fragrans Houtt mace extract. The cytotoxic activity of the Myristica fragrans Houtt mace acetone extract was assayed by MTT assay on human oral epidermal carcinoma KB cell lines. KB cells were incubated with different concentration of mace extract ranging from 25 to 125 μg/mL for 24hrs. The apoptotic induction potential was also studied by the analysis of Bcl-2 protein and gene expression in mace extract incubated KB cell lines using western blotting technique and real-time polymerase chain reaction. The mace extract exhibited cytotoxicity and anticancer effect against KB cell lines and it also suppressed the growth of cancer cells, therefore growth inhibitory effect was noted in extract treated cell lines. The apoptotic potential of mace extract was accompanied by reduced gene expression of Bcl-2 compared to the untreated KB cells. The mace extract shows the cytotoxic activity and induced the apoptosis through the modulation of its target genes Bcl-2 in the KB cell lines, suggesting the potential of mace as a candidate for oral cancer chemoprevention. This can be further investigated in vivo for its anticancer potential.

Mixed natural arylolefin-quinoline platinum(II) complexes: synthesis, structural characterization and in vitro cytotoxicity studies.

Five new platinum(II) complexes bearing a eugenol and a quinoline derivative, namely [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]-trans-dichlorido(quinoline-κN)platinum(II), [PtCl2(C15H20O4)(C9H7N)], (2), {η2-4-allyl-2-methoxy-1-[(propan-2-yloxy)carbonylmethoxy]benzene}-trans-dichlorido(quinoline-κN)platinum(II), [PtCl2(C15H19O4)(C9H7N)], (3), [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]chlorido(quinolin-8-olato-κ2N,O)platinum(II), [Pt(C9H6NO)Cl(C15H20O4)], (4), {η2-4-allyl-2-methoxy-1-[(propan-2-yloxy)carbonylmethoxy]benzene}chlorido(quinolin-8-olato-κ2N,O)platinum(II), [Pt(C9H6NO)Cl(C15H20O4)], (5), and [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]chlorido(quinolin-2-carboxylato-κ2N,O)platinum(II), [Pt(C10H6NO2)Cl(C15H20O4)], (6), have been synthesized and fully characterized spectroscopically. A single-crystal X-ray diffraction study was carried out for complexes (2) and (4)-(6). PrEug [or 4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene] in (2), (4) and (6), and iPrEug (the propan-2-yloxy analogue of PrEug) in (3) and (5) coordinate with PtII at the ethylenic double bond of the allyl group. In (2)-(6), the donor N atom of the amine group occupies a trans position with respect to the double bond. A comparison of the IC50 values of 0.38-29.23 µM for (2)-(6) with cisplatin, as well as other platinum(II) complexes, indicates an excellent in vitro cytotoxicity against the KB, LU, Hep-G2 and MCF-7 cancer cell lines, with the highest cytotoxic effect (IC50 = 0.38-1.99 µM) being for complexes (4) and (5) bearing a quinolin-8-olate ligand.

Bioactive xanthoquinodins and epipolythiodioxopiperazines from Chaetomium globosum 7s-1, an endophytic fungus isolated from Rhapis cochinchinensis (Lour.) Mart

A new xanthoquinodin B9 (1), together with two known xanthoquinodins, xanthoquinodin A1 (2) and xanthoquinodin A3 (3), three epipolythiodioxopiperazines, chetomin (4), chaetocochin C (5) and dethio-tetra(methylthio)chetomin (6), and four other compounds, chrysophanol (7), emodin (8), alatinone (9), and ergosterol (10) were isolated from the endophytic fungus Chaetomium globosum 7s-1, isolated from Rhapis cochinchinensis (Lour.) Mart. All isolated structures were established based on their spectroscopic data analyses. Compounds 1–6 showed antibacterial activity against Gram positive bacteria with MICs ranging from 0.02 pM to 10.81 µM. Compounds 1–6 also exhibited cytotoxicity against KB, MCF-7 and NCI-H187 cancer cell lines (IC50 0.04–18.40 µM). However, they were cytotoxic towards a normal cell line (Vero cell) with IC50 values ranging from 0.04 to 3.86 µM.

Evaluating the photodynamic therapy efficacy using 5-aminolevulinic acid and folic acid-conjugated bismuth oxide nanoparticles on human nasopharyngeal carcinoma cell line

Selective accumulation of photosensitizers (PSs) into cancerous cells is one of the most important factors affecting photodynamic therapy (PDT) efficacy. 5-Aminolevulinic acid (5-ALA) is precursor of a strong PS, protoporphyrin-IX (Pp-IX); but it has poor permeability in lipophilic membrane of the cells due to its hydrophilic property. Therefore, establishment of an improved delivery strategy could highly affect on treatment outcome. Moreover, folate receptors (FRs) are overexpressed on the surface of many tumor cells. In the present work, targeting ligand folic acid (FA) and 5-ALA conjugated bismuth oxide nanoparticles (FA-5ALA-Bi2O3 NPs) were synthesized; and used in PDT against human nasopharyngeal carcinoma cells (KB cell line). The KB cells incubated with the synthesized NPs for 2 h; then illuminated using a custom-made red light LED lamp at the light dose of 26 J/cm2. MTT and caspase-3 activity assays were performed to evaluate the efficacy of treatment. Results showed that FR targeting ligand enables selective endocytosis of FA-5-ALA-conjugated NPs into KB cells. Improved internalization of 5-ALA into cells decreased the cell viability to about 50%, 65%, and 85% in the groups receiving FA-5ALA-Bi2O3 NPs, 5ALA-Bi2O3 NPs, free 5-ALA and subsequent PDT, respectively. Therefore, FA-5ALA-Bi2O3 NPs can significantly increase the cell killing effect of PDT.

Natural anti-proliferative agent loaded self-microemulsifying nanoparticles for potential therapy in oral squamous carcinoma

Piperine is a poorly water-soluble drug and its bioavailability is a great barrier for this drug. The objective of current work was to formulate and investigate a self-microemulsifying drug delivery system (SMEDDS) of piperine as well as modification of liquid SMEDDS into the solid SMEDDS. Solubility study of piperine was performed in various excipients. Optimum composition of the microemulsion region was identified by using the pseudo-ternary phase diagram. Liquid SMEDDS formulation was optimized by Box–Behnken statistical design. The optimized liquid SMEDDS formulation showed particle size 22.12 ± 0.88 nm, PDI 0.185 ± 0.03 and transmittance 99.48 ± 0.32%. A methyl thiazolyl tetrazolium (MTT) assay was performed to determine in vitro anticancer efficacy of piperine using KB cell lines. The piperine loaded self-microemulsifying nanoparticles significantly inhibited the growth of carcinoma cells by targeting mitochondria and produced caspases-3 activity. Whereas, this mechanism showed significant role in inhibition of cancer signaling stage. The MTT assay confirmed 98.7% cytotoxicity in cancerous cells. Moreover, PXRD analysis showed the transformation of the crystalline structure of piperine to the amorphous (dissolved) state. In vitro release and ex vivo permeation of liquid and solid-SMEDDS has shown faster drug release as compared to the pure drug. The developed formulation was stable under stability conditions after 3 months of storage. Thus, the studies revealed that SMEDDS has a promising strategy for a poorly water-soluble drug, which benefits to enhance the solubility, dissolution also an anti-proliferative performance of piperine in the oral squamous carcinoma.

D-Gluconic acid–based methotrexate prodrug–loaded mixed micelles composed of MDR reversing copolymer: in vitro and in vivo results

The main aim of the present research was to synthesize carbohydrate (d-gluconic acid, DGA) prodrug of methotrexate (MTX) to improve the aqueous solubility and to develop mixed micelles (MMs) composed of d-α-tocopheryl poly (ethylene glycol) 1000 succinate (TPGS) as an MDR reversing copolymer and poloxamer 407 (P-407) to deliver the MTX prodrug to tumor tissue via enhanced permeability and retention (EPR) mechanism. MTX-DGA conjugate (MDGAC) was synthesized using Steglich esterification reaction. The MDGAC-loaded TPGS and P-407 MMs (MDGAC-TP MMs) were prepared by solvent evaporation technique. MDGAC-TP MMs showed low critical micelle concentration, high drug loading, sustained release profile, lower hemolytic behavior, higher in vitro cytotoxicity against the human carcinoma cell lines KB and MDR KBv, and significantly reduced in vivo toxicity. Therefore, the developed MDGAC-TP MMs could be a promising and effective approach for the development and treatment of MDR tumors.

CYTOTOXICITY OF STRAWBERRY EXTRACT ON ORAL CANCER CELL LINE

Objective: Berries including strawberry may have beneficial effects against oxidative stress-mediated diseases such as cancer. The purpose of the present study was to investigate the cytotoxic effects of strawberry extract on oral cancer cell line.Methods: Strawberry methanolic extract (SBE) was prepared, and cytotoxic activity of different concentration of SBE on KB cell lines was determined by (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay and neutral red dye incorporation test.Results: Strawberry extract exhibits cytotoxic activity over the oral cancer cell lines. On administration of about 100 μg/ml of strawberry extract, about 50% of cell viability could be observed and assessed from the cell lines.Conclusion: Strawberries have a cytotoxic effect on oral cancer cell line due to the presence of anticancer constituents in the berries. These berries can be used as a natural medicine for cancer sufferers.

New neolignans from the seeds of Myristica fragrans and their cytotoxic activities.

Three new dihydrobenzofuran neolignans, myticaganal A-C (1-3), along with five known compounds (4-8), were isolated from the seeds of Myristica fragrans. Their structures were elucidated by extensive spectroscopic analysis. In vitro cytotoxic activities of the isolated compounds against three human cancer cell lines (KB, oral cavity; MCF-7, breast cancer; and NCI-H187, small cell lung cancer) were evaluated. Neolignan 3 showed significant cytotoxicity against KB and NCI-H187 cell lines with IC50 values of 5.9 and 6.3μM, respectively.

SECOND METABOLITES AND ANTIOXIDANT, ANTIMICROBIAL, ANTICANCER ACTIVITIES OF <i>Helicteres hirsuta</i> ROOT EXTRACT

Helicteres hirsuta Lour., particularly its stems and leaves have been used in 
 Vietnamese traditional medicine to cure furuncles, dysentery, measles and flu. In this study, we examined biological activities of 5 fractions from methanol extract of H. hirsuta roots. The results showed that ethyl acetate fraction has the highest content of phenolic and flavonoid compounds (220.9 ± 15.67 mg GAE, gallic acid equivalents /g dry weight and 23.03 ± 0.97 mg QE, quercetin equivalents /g dry weight, respectively). Fractions from H. hirsuta roots exhibited antioxidant, an-tibacterial and anticancer activities. Ethyl acetate fraction showed the strongest antioxidant activi-ty through 1,1diphenyl-2-picrylhydrazyl (DPPH) scavenging capacity (half-maximal inhibitory concentration, IC50 value of 0.117 ± 0.023 mg/ml). Ethyl acetate fraction of roots also showed the strongest reducing power (0.071 ± 0.009 mg/ml) and cytotoxicity on human KB cell lines (IC50= 3.23 μg/ml). Besides, fractions from H. hirsuta roots had high inhibitory activity against Gram-positive bacteria namely Staphylococcus aureus and Lactobacillus fermentum. The results suggest potential exploitation of bioactive compounds from H. hirsuta roots especially ethyl acetate frac-tion and its application in medicine and pharmacy. This is the first report on second metabolite composition and biological activities of H. hirsuta roots.

Flavonoids from Milletia leucantha and Their Cytotoxicity

Two known chalcones (1–2), five known flavonol derivatives (3 and 5–8) and one flavone (4) were isolated for the first time from fruits of Millettia leucantha Kurz. In addition, 5 was found for the first time from this genus. Their structures were elucidated on the basis of IR, MS, 1D and 2D NMR techniques. Chalcone 1 exhibited moderate cytotoxicity against the MCF-7 cell line with an IC50 value of 50.93 μM, whereas this compound showed inactive cytotoxicity against Vero cells. Compound 2 exhibited cytotoxicity against the KB, NCI-H187 and Vero cell lines with IC50 values of 63.64, 114.44 and 28.44 μM, respectively. Compound 8 only showed cytotoxic activity against the KB cell line with an IC50 value of 110.23 μM.

Cytotoxic Evaluation of Compounds Isolated from the Aerial Parts of Hedyotis pilulifera and Methanol Extract of Inonotus obliquus

The aim of this study was to evaluate the inhibitory activity of compounds isolated from the aerial parts of Hedyotis pilulifera (Pit.) T.N. Ninh toward selected cancer cell lines. The isolated compounds were identified by analyzing their nuclear magnetic resonance spectral data and physical properties, and comparison of these with reported data. The sulforhodamine B assay was used for the cytotoxic evaluation of isolates. Among twenty-one compounds isolated from H. pilulifera, compounds 2, 3, and 4 showed moderate inhibitory effect on MCF-7 with IC50 values of 63.5, 59.4, and 52.7 μg/mL, respectively, while the other compounds exhibited no effect (IC50 values > 100 μg/mL). Further investigation using HT29, LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines showed the moderate cytotoxic activity of compound 3 (IC50 values ranging from 51.7 to 78.3 μg/mL) to all cells, while compound 4 showed selective effect only against HL-60 cells (IC50 61.5 μg/mL). This is the first report of cytotoxic activity of pomolic acid 3β-acetate (3) toward all tested cancer cell lines, and also the first report of cytotoxicity of rotungenic acid (4) against LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines. The methanol extract of chaga mushroom { Inonotus obliquus (Ach. ex Pers.) Pilát} exhibited the strongest cytotoxic effects against HL-60 and LU-1 (32.2 and 38.0 μg/mL, respectively), and modest cytotoxic effects against SW480 (41.3 μg/mL), HepG2 (51.3 μg/mL), KB (57.0 μg/mL), and LNCaP (57.7 μg/mL). We conclude that compounds 3 and 4 from H. pilulifera may be useful in further investigation for anticancer agent discovery and chaga could be used as a natural anticancer remedy against promyelocytic leukemia and lung adenocarcinoma.

Synthesis and Cytotoxic Evaluation of Artemisinin Derivatives Containing an Aminopropanol Group

Series of novel artemisinin derivatives were designed and synthesized in which the amino propanol group was bonded to the artemisinin nucleus through C-C linkage. Ten new compounds were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.

Design, Synthesis and Cytotoxic Evaluation of Novel Lupane Triterpenoid and Ursolic Acid Derived 2-Aminobenzamides

Series of novel triterpenoid hybrids were designed and synthesized by introducing 2-aminobenzamide moiety at C28 position of triterpenoid derivatives. Thirteen new conjugates were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.

Elucidation of the Relationship between CD Cotton Effects and the Absolute Configuration of Sixteen Stereoisomers of Spiroheterocyclic-Lactams.

As part of research to search for antitumor agents in fungi originating from marine organisms, cephalimysins E–L were isolated from a culture broth of Aspergillus fumigatus that was separated from the marine fish Mugil cephalus. One- and two-dimensional nuclear magnetic resonance spectra revealed their planar structures, which are diastereomers of each other. Their absolute stereostructures were established by epimerization at C-8 with acidic methanol, nuclear Overhauser effect spectroscopy (NOESY), and circular dichroism (CD) spectroscopy. These demonstrated the detailed relationships between absolute configuration and CD Cotton effects. Additionally, in the growth inhibition assay against P388, HL-60, L1210, and KB cell lines, some of the fungal metabolites or reaction products exhibited moderate activities.

Synthesis, structure and in vitro cytotoxicity testing of some 1,3,4-oxadiazoline derivatives from 2-hydroxy-5-iodobenzoic acid.

The syntheses of nine new 5-iodosalicylic acid-based 1,3,4-oxadiazoline derivatives starting from methyl salicylate are described. These compounds are 2-[4-acetyl-5-methyl-5-(3-nitrophenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6a), 2-[4-acetyl-5-methyl-5-(4-nitrophenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6b), 2-(4-acetyl-5-methyl-5-phenyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)-4-iodophenyl acetate, C19H17IN2O4 (6c), 2-[4-acetyl-5-(4-fluorophenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate, C19H16FIN2O4 (6d), 2-[4-acetyl-5-(4-chlorophenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate, C19H16ClIN2O4 (6e), 2-[4-acetyl-5-(3-bromophenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6f), 2-[4-acetyl-5-(4-bromophenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6g), 2-[4-acetyl-5-methyl-5-(4-methylphenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6h) and 2-[5-(4-acetamidophenyl)-4-acetyl-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl]-4-iodophenyl acetate (6i). The compounds were characterized by mass, 1H NMR and 13C NMR spectroscopies. Single-crystal X-ray diffraction studies were also carried out for 6c, 6d and 6e. Compounds 6c and 6d are isomorphous, with the 1,3,4-oxadiazoline ring having an envelope conformation, where the disubstituted C atom is the flap. The packing is determined by C-H...O, C-H...π and I...π interactions. For 6e, the 1,3,4-oxadiazoline ring is almost planar. In the packing, Cl...π interactions are observed, while the I atom is not involved in short interactions. Compounds 6d, 6e, 6f and 6h show good inhibiting abilities on the human cancer cell lines KB and Hep-G2, with IC50 values of 0.9-4.5 µM.

Two new 18, 19-seco Triterpenoids from Ilex asprella (Hook. et Arn.) Champ. ex Benth

Two novel 18,19-seco-ursane triterpenoid saponins, ilexasprellanosides J–K (1–2, resp.), 3-O-α-l-Rhamnopyranosyl-(1 → 2)-β-d-xylopyrannosyl-19-O-β-d-glucopyranosyl-16-β-hydroxyl-18,19-seco-13(18)-urs-ene-21, 28-lactone (1), 3-O-β-d-Xylopyrannosyl-19-O-α-l-rhamnopyran osyl-(1 → 2)-α-l-arabinopyranoside-16, 21-epoxy-18, 19-seco-13(18)-urs-ene-28-oic acid (2), five known compounds (3–7) were isolated from the leaves of Ilex asprella (Hook. et Arn.) Champ. ex Benth. (Gangmeiye). The chemical structures of these compounds were elucidated through UV, IR, ESI-MS, 1H NMR and 13C NMR analyses. In MTT and SRB assays, compounds 1–4 presented cytotoxic activities against several human cancer cell lines, namely, the HL-60 human acute promyelocytic leukaemia, Bel 7402 liver cancer, BGC-823 gastric cancer and KB human nasopharyngeal carcinoma cell lines. Compound 1 exhibited weak cytotoxic activities against the human tumour cell lines HL-60, Bel 7402 and KB with inhibition rates of 27.97%, 21.00% and 25.60%, respectively. Compound 2 exhibited weak cytotoxic activities against the human tumour cell lines HL-60, Bel 7402 and BGC-823 with inhibition rates of 19.34%, 7.50% and 4.26%. Respectively, the compounds exerted no statistically different effects on mast cell degranulation in rats. This result indicates that the compounds do not affect mast cell degranulation

Synthesis of asiatic acid derivatives and their cytotoxic activity

Twenty-eight compounds, including 24 new (4–22, 25–26, and 28–30) and four known (2, 23, 24, and 27) have been synthesized starting from asiatic acid (1), which was isolated from Centella asiatica. The preparation procedure included the acetylation, hydrolyzation on the 2-, 3-, 23-, and the side chain hydroxyl, amino groups, as well as the amidation of the 28-carboxylic group. All the synthesized derivatives were structurally confirmed by 1H, 13C NMR, and MS spectra. Besides, they were evaluated for their cytotoxicity against three cancer cell lines: KB (human carcinoma in the mouth), HepG2 (human hepatocellular carcinoma), and SK-LU-1 (human lung carcinoma). Eleven of the tested compounds, including nine newly synthesized and two known ones showed very strong activity against three tested cell lines with the IC50 values ranging from 0.67 to 37.39 µM. Three compounds showed good activity against KB and HepG2 cell lines with the IC50 values ranging from 1.95 to 32.12 µM. The activity against the KB and HepG2 cell lines was in general higher than that against the SK-LU-1 cell line. The acetylation of the hydroxyl groups in the A-ring and the OH or NH groups in the amide side chains strongly enhanced the activity of the compounds. In addition, five potent compounds (9, 12, and 15–17) were also evaluated for apoptosis-inducing activities. The ratio of apoptosis and necrotic cells increased when lung cancer cells were treated with these compounds. On the other hand, compound 9 increased caspase 3 activities (P < 0.05). Thus, these compounds induced lung cancer cell death by apoptosis and necrosis.

Synthesis of novel artemisinin–triazole hybrids

AbstractSeveral substituted triazole–artemisinin hybrids were synthesized based on ‘click’ chemistry between propargyl‐substituted derivatives and artemisinin containing a 2‐hydroxypropane unit. The structures of all obtained compounds were confirmed by means of IR, NMR, and MS spectroscopy. Four new hybrids were evaluated as cytotoxic agents, revealing an interesting anticancer activity of 1‐(4‐(3‐Aminophenyl)‐1H‐1,2,3‐triazol‐1‐yl)‐3‐(((3R,6R,8aS,9R,10S,12R,12aR)‐3,6,9‐trimethyl‐decahydro‐12H‐3,12‐epoxy[1,2]dioxepino[4,3‐i]isochromen‐10‐yl)oxy)propan‐2‐ol compound in KB and HepG2 cancer cell lines.