Good Cytotoxic Activity Research Articles

Synthesis of Bioactive N‐Acyclic Gold(I) and Gold(III) Diamino Carbenes with Different Ancillary Ligands

A series of gold(I) and gold(III) N‐acyclic diamino carbene (ADC) complexes with different ancillary ligands have been synthesized. The chloride carbene derivatives [Au{C(NHR)(NHCH2py)}Cl] (R = Cy, R = naphthyl, R = xylyl) have been obtained by reaction of 2‐picolylamine with the corresponding [AuCl(CNR)]. The gold(I) thiolate derivatives [Au{C(NHR)(NHCH2py)}(Spy)] were prepared by reaction of the chlorido complexes with 2‐mercaptopyridine (2‐HSpy) in presence of potassium carbonate. The phosphane derivative [Au(pyCH2NH2)(PPh3)](OTf) was obtained by reaction of freshly prepared [Au(OTf)(PPh3)] with 2‐picolylamine. The phosphane‐carbene complexes [Au{C(NHR)(NHCH2py}(PPh3)](OTf) were obtained from the reaction of picolylamino species with the isocyanide. The gold(III) derivative cis‐[Au(C6F5)2(pyCH2NH2)](ClO4) was obtained by the reaction of 2‐picolylamine with freshly [Au(C6F5)2(Et2O)2](ClO4). The reaction of the former with CNCy led to complex cis‐[Au(C6F5)2{C(NHCy)(NHCH2py)}]ClO4 by a nucleophilic attack of the isocyanide to the amine ligand, thus producing a bidentate C,N acyclic carbene ligand. Cytotoxic studies against the tumor human cell lines Jurkat (T‐cell leukaemia), MiaPaca2 (pancreatic carcinoma), A549 (lung carcinoma) and MDA‐MB‐231 (breast carcinoma) showed moderate to good cytotoxic activity for some of the complexes.

IN VITRO ANTIOXIDANT AND CYTOTOXIC PROPERTIES OF FUCOIDAN FROM THREE INDIAN BROWN SEAWEEDS

Objective: In the present study, fucoidan extracted from three brown algae, Sargassum wightii, Turbinaria ornata, and Padina tetrastromatica, was purified, characterized, and evaluated for antioxidant and cytotoxic properties.
 Methods: Algal powders were sequentially extracted with five solvents based on polarity and residue was subjected to acidic extraction. The filtrates were precipitated for alginates, and resultant supernatant was precipitated for fucoidan. The precipitate was centrifuged; pellet dialyzed and lyophilized to yield crude fucoidan, which was purified by diethylaminoethyl cellulose chromatography and characterized by biochemical tests and Fourier-transform infrared (FT-IR) spectrometry. Solvent extracts and fucoidans were subjected to 2,2-diphenyl-1-picrylhydrazyl assay. Fucoidans were subjected to trypan blue cytotoxicity assay.
 Results: Antioxidant activity was highest in methanol extracts and Padina crude fucoidan, while lowest in hexane extracts and purified Sargassum fucoidan. Sargassum yielded the highest amount of fucoidan (7.14%). Total carbohydrates increased as Sargassum> Padina > Turbinaria, sulfates as Padina > Turbinaria > Sargassum, and protein content was 0.16±0.001%. Cytotoxicity increased in a dose-dependent manner; the highest and lowest for Padina at 200 mg mL-1 (40%) and 10 mg mL-1 (4%), respectively. Antioxidant and cytotoxic properties exhibited a positive correlation with sulfate content. FT-IR spectral values were characteristic to fucoidan.
 Conclusion: Fucoidans from the three algae effectively scavenged free radicals and showed good cytotoxic activity. There was a positive correlation between sulfate content and bioactivity of fucoidans, supporting its structure-function relationship. Thus, extracts and fucoidans from these algae are found to be potential candidates for pharmacological applications.

Synthesis, Crystal Structure, DNA Binding, and Cytotoxicity of a Zn(II) Complex Constructed from Phenylacetic Acid

A novel Zn(II) complex with the formula {[ZnL2(dibe)2]·2H2O}n (synthesized using a carboxylic acid ligand, L = phenylacetic acid, dibe = 4,4′-bipyridine (bipy)) is synthesized at room temperature, characterized and its DNA binding, cleavage, anticancer properties are studied by elemental analysis, infrared spectroscopy, and single crystal X-ray diffraction. The interaction of the complex with fish sperm DNA (FS-DNA) is monitored, which reveals that the complex has the ability to bind to FS-DNA. The complex is further studied for the gel electrophoresis assay with supercoiled plasmid pBR322 DNA. In addition, anticancer activities of the metal complex investigated through MTT in vitro assays, indicate that the complex shows good cytotoxic activity against cancer cell lines. Flow cytometry and apoptosis experiments show that the complex induces apoptosis of HeLa cells, which demonstrates that the complex exhibits a significant cancer cell inhibitory rate.

Cytotoxic glycosides from the roots of Weigela x “Bristol Ruby”

Seven oleanane-type glycosides were extracted and isolated by various chromatographic methods from the roots of Weigela x “Bristol Ruby” (1–7), six previously undescribed (1–6) and a known one (7). Their structures were assigned by spectroscopic analysis mainly 2D NMR and mass spectrometry (ESIMS). Selected triterpenoid glycosides (1–3, 6, 7) displayed a good cytotoxic activity against a mouse colon cancer cell line CT26.

Design, Synthesis and Anticancer Evaluation of Novel Series of Indibulin Analogues.

Cancer is an important cause of human death worldwide. During the last decades, many anticancer agents with anti-tubulin mechanism have been synthesized or extracted from nature and some of them also entered clinical use. Indibulin is one of the most potent tubulin polymerization inhibitors with minimal peripheral neuropathy, which is a big problem by some of the antimitotic agents such as taxanes and vinka alkaloids. With respect to this giant benefit, herein we decided to design and synthesize novel indibulin related compounds and investigate their anticancer activity against HT-29, Caco-2 and T47-D cancerous cell lines as well as NIH-T3T as normal cell line. The aim of this study was to synthesize new anti-cancer agents and evaluates their cytotoxic activity on diverse cancerous and normal cell lines. Target compounds were synthesized in multistep reaction and cytotoxic activity was investigated by MTT cell viability assay. Herein, nine novel target compounds were synthesized in moderate to good yield. Some of the compounds exerted good cytotoxic activity against cancerous cell lines. Annexin V/PI staining showed that compound 4g could induce apoptosis and necrosis in HT-29 cell line. It is valuable to do further investigation on compound 4g which showed the highest activity against HT-29 and Caco-2 (IC50 values are 6.9 and 7 µM respectively). Also, synthesis of new derivatives of current synthesized compounds is suggested.

The Genus Glycosmis [Rutaceae]: A Comprehensive Review on its Phytochemical and Pharmacological Perspectives

Background:Medicinal plants are rich source of large variety of lead compounds. The plants of genus Glycosmis or its different parts valued for its therapeutic and medicinal qualities. Glycosmis belongs to the family Rutaceae.Objective:The genus Glycosmis is a rich source of pharmacologically and biologically active secondary metabolites, such as alkaloids, flavonoids, phenolic glycosides, quinones, terpenoids, glycerides isolated from different parts of Glycosmis plant. The objectives of this review is to provide updatedand complete information on the distribution, phytochemical, pharmacological, and toxicity research of Glycosmis species.Results:About 233 phytoconstituents are isolated from this genus. Recent interest in this genus has focused on isolating and identifying of different phytoconstituents that exhibit potent antioxidant, antibacterial, antiviral and anticancer activities. They show good cytotoxic activity against various cancer cell lines and also reported for good antiviral and immunomodulatory activity. In this support convincing evidence in experimental animal models are available.Conclusion:This review summarizes information about the isolated compounds their bioactivities related to same compounds present in other plants including pharmacological activities of plant extract of Glycosmis genus.

Pumilaside A from Litchi semen induces apoptosis in human gastric cancer BGC823 cells via activation of death receptor- and mitochondria-mediated apoptotic pathways

Purpose: To investigate the cytotoxic effect of pumilaside A from Litchi semen against human gastric cancer BGC823 cells, and unravel its possible mechanism(s) of action.Methods: The cytotoxic activity of pumilaside A (5 - 40 μg/mL) against BGC823 cells was assessed by thiazolyl blue tetrazolium bromide assay. The pro-apoptotic effect of PA (10, 20 or 40 μg/mL) on BGC823 cells was monitored by flow cytometry, while the mechanisms involved were investigated using western blot.Results: Pumilaside A significantly produced cytotoxic activity against BGC823 cells (IC50 = 25.43 μg/mL) and induced apoptosis in BGC823 cells (p < 0.01). Treatment with pumilaside A led to significant upregulation of pro-apoptotic factors (Fas, FasL, FADD, Bax, Apaf-1, and c-caspase -8, 9 and 10), and downregulation of anti-apoptotic factors (survivin and Bcl-2, p < 0.05, 0.01). In addition, pumilaside A increased the cytoplasmic levels of Smac and cytochrome c in BGC823 cells by enhancing their mitochondrial release, and significantly upregulated the levels of executioner c-caspases-3, 6 and 7 (p < 0.05, 0.01).Conclusion: Pumilaside A shows good cytotoxic activity against BGC823 cells via a mechanism related to activation of death receptor- and mitochondria-mediated apoptotic pathways. Thus, pumilaside A has a potential for use as an anti-gastric cancer agent.Keywords: Litchi semen, Pumilaside A, BGC823 cells, Cytotoxicity, Apoptosis

Synthesis and biological evaluation of marine alkaloid-oriented β-carboline analogues

Pityriacitrin is a marine alkaloid with typical β-carboline scaffold, and which has been proven to exhibit diverse biological functions. During the course of our research for highly active compounds from natural products, the pityriacitrin have also been isolated and identified from a Chinese Burkholderia sp. NBF227. So, in order to explore the potential functional molecules, a series of β-carboline analogues derived from pityriacitrin were designed and synthesized, and their in vitro cytotoxic activities against SGC-7901, A875, HepG2, and MARC145 cell lines were evaluated. The results demonstrated that some of these β-carboline derivatives exhibited moderate to good cytotoxic activities, especially, compound 9o with a special sulfonyl group presented the highest inhibitory activities against all tested cell lines with the IC50 values of 6.82 ± 0.98, 8.43 ± 1.93, 7.69 ± 2.17, 7.19 ± 1.43 μM, respectively, which might be used as lead compound for discovery of novel cytotoxic agents.

One-Pot Synthesis of Triazolo-Heterolignans: Biological Evaluation and Molecular Docking Studies as Tubulin Inhibitors.

The anti-mitotic activity of podophyllotoxin derivative targeting tubulin enzyme proved them as strong polymerization inhibitors. The introduction of heteroatom along with different heteroaryl systems in naturally obtained lignans created a latitude for design of bioactive components. A novel one-pot sequential propargylation/cycloaddition reaction strategy has been followed to synthesize triazolo-heterolignans. To screen anti-proliferative activity of novel heterolignans and to determine their mode of action. SRB assay, Cytotoxicity evaluation, PI uptake for analysis of cell cycle, caspase-3 activity, Western blot analysis and Immunofluorescence and molecular docking studies. SRB assay of synthesised compounds were provided compound 3a and 5f to be highly active among the synthesized compounds. The Compound 3a showed cell cycle arrest at G2/M phase and 5f arrest the cells at G1 phase. Compound 5f displayed caspase 3 mediated apoptotic effect at lower levels. Compound 3a and 5f displayed microtubule disassembly inhibition same as paclitaxel and found to be occupying colchicine binding site of tubulin, both ligands were depicted π-cation interaction with Lys352 residue and triazole ring accommodated at the lactone binding site. A novel one-pot sequential propargylation/cycloaddition reaction has been developed for the synthesis of triazolo-heterolignans. Compound 3a and 5f were displayed good cytotoxic activities and found to inhibit microtubule disassembly. The importance of triazole ring of heterolignans has been studied by molecular docking experiments and results were compared.

Mitochondria-localizing N-heterocyclic thiosemicarbazone copper complexes with good cytotoxicity and high antimetastatic activity

Although many N-heterocyclic thiosemicarbazone copper complexes have been proposed as potential anticancer agents, little is known about their intracellular localization in cells. In the present study, we synthesized two fluorescent N-heterocyclic thiosemicarbazone copper complexes, ([CuII(L)(Br)] 1 and [CuII2CuI(L)2(Br)3] 2, where HL is (E)-N,N-dimethyl-2-(quinolin-8-ylmethylene)hydrazinecarbothioamide), to assess their intracellular distribution. Our fluorescence studies demonstrated that complex 1 showed an intense emission band at ca. 510 nm (λex = 405 nm) similar to that of complex 2, albeit with about four times lower emission intensity. Both copper complexes showed significantly greater cytotoxicity toward several tumor cell-types with better IC50 (0.27–0.91 μM) than the HL ligand and cisplatin. Scratching wound healing assay and invasion assay were performed, revealing that the copper complexes have good antimetastatic activity. Confocal fluorescence imaging allowed ascertaining that complex 2 was primarily localized to mitochondria. Further studies revealed that the anticancer mechanisms of complex 2 might involve the mitochondrial-mediated apoptotic pathway, probably caused by the reducing mitochondrial membrane potential and induction of ROS (reactive oxygen species) production. Furthermore, complex 2 exhibited promising cytostatic effects in a three-dimensional HeLa spheroid model.

Structure and cytotoxicity of zinc (II) and cobalt (II) complexes based on 1,3,5‐tris(1‐imidazolyl) benzene

Three novel complexes, [Zn (tib)2·(H2O)2]·(NO3)2 (1), [Co (tib)2]·2NO3 (2) and [Co2(tib)2(btc)]·H2O (3) [H4btc = 1,2,4,5‐benzenetetracarboxylic acid; H2tib = 1,3,5‐tris(1‐imidazolyl)benzene], were synthesized and characterized by single‐crystal X‐ray, IR and elemental analysis. The interaction of these complexes with FS‐DNA (fish sperm DNA) was monitored, and binding constants were determined using UV/Vis, which revealed that they have the ability to bind to FS‐DNA. DNA‐binding constants (K) for the three complexes were 2.2 × 104 m−1, 0.7 × 104 m−1 and 0.09 × 104 m−1, respectively. The interaction capacity of the complexes with FS‐DNA has been investigated by fluorescence spectroscopy. Stern–Volmer quenching plot values for complexes 1, 2 and 3 were 0.3784, 0.1028 and 0.076, respectively. The viscosity measurement suggested that complexes 1, 2 and 3 interact with DNA in an intercalation mode. In addition, anti‐cancer activities of these complexes investigated through MTT assays in vitro indicated that the complexes showed good cytotoxic activity against cancer cell lines. Cytotoxic activity of test complexes against two different cancer cell lines (HeLa and KB cells) showed significant cancer cell inhibition rates. Flow cytometry experiments and morphological apoptosis studies showed that the complexes induced apoptosis of HeLa tumor cell lines. Finally, a further molecular docking technique was employed to confirm the binding of the complexes toward the molecular target DNA.

A Rapid and Convenient Synthesis of Acridine Derivatives Using Camphor Sulfonic Acid Catalyst

Acridines were first developed as dyes, and since the early 20th century their varied properties have continued to be of interested. Derivatives of acridine showed good cytotoxic activity against h...

Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone

Steroids are classes of natural products widely distributed in nature, which have been demonstrated to exhibit broad biological functions, and have also attracted increasing interest from bioorganic and pharmaceutical researches. In order to develop novel chemical entities as potential cytotoxic agents, a series of steroidal isatin conjugations derived from epiandrosterone and androsterone were efficiently prepared and characterized, and all these obtained compounds were screened for their potential cytotoxic activities. The preliminary bioassay indicated that most of the newly synthesized compounds exhibited good cytotoxic activities against human gastric cancer (SGC-7901), melanoma (A875), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), which might be considered as promising scaffold for further development of potential anticancer agents.

Synthesis and cytotoxic evaluation of novel quinozalinone derivatives with substituted benzimidazole in position 3.

Quinazolinone and benzimidazole are both fused heterocyclic compounds which have shown valuable biological properties including cytotoxic, antibacterial, and antifungal activities. In this study, a series of novel quinazolinone derivatives substituted with benzimidazole were synthesized in two parts. In the first part 2 - phenyl - 1H - benzimidazol - 6 - amine (4) was synthesized from the reaction of 4-nitro-o-phenylenediamine and benzoic acid. In the second part, new 3-(2-phenyl-1H benzoimidazol-5-yl)- 3H-quinazolin-4-one derivatives (8a-8f) were also prepared. Finally compound 4 was reacted with the different benzoxazinone derivatives (8a-8f) to give the target compounds. The structures of the synthesized compounds were confirmed by IR and 1HNMR. Cytotoxic activities of the final compounds were assessed at 100, 200, 300, 400, and 500 μM against MCF-7 and HeLa cell lines using the MTT colorimetric assay. Almost all compounds exhibited good cytotoxic activity against both cell lines. Compound 9d demonstrated the highest cytotoxic activity against MCF7 and Hela cell lines with IC50 70 μM and 50 μM, respectively.

Synthesis, crystal structure, DNA binding, and cytotoxicity of a Zn(II) complex constructed from phenylacetic acid

A novel Zn(II) complex with the formula {[ZnL2(dibe)2]⋅2H2O}n (synthesized using a carbo­xylic acid ligand, L = phenylacetic acid, dibe = 4,4'-bipyridine (bipy)) is synthesized at room temperature, characterized and its DNA binding, cleavage, anticancer properties are studied by elemental analysis, infrared spectroscopy, and single crystal X-ray diffraction. The interaction of the complex with fish sperm DNA (FS-DNA) is monitored, which reveals that the complex has the ability to bind to FS-DNA. The complex is further studied for the gel electrophoresis assay with supercoiled plasmid pBR322 DNA. In addition, anticancer activities of the metal complex investigated through MTT in vitro assays, indicate that the complex shows good cytotoxic activity against cancer cell lines. Flow cytometry and apoptosis experiments show that the complex induces apoptosis of HeLa cells, which demonstrates that the complex exhibits a significant cancer cell inhibitory rate.

Synthesis, crystal structure, DFT study, in vitro and in silico molecular docking of novel bis (aroyl selenourea) derivatives

A new family of o-phenylenediamine substituted bis (aroyl selenourea) 1–3 were synthesised and characterised by spectroscopic methods and Single crystal XRD studies. The 1–3 showed that the synthesised compounds in crystallise in the monoclinic crystal system, and space group present is P 2/c, C 2/c and P 21/c. The computational studies of 1–3 were performed with Density function theory (DFT) using B3LYP/6-31G (d, p) level of theory. Molecular electrostatic potential map (MEP) and frontier molecular orbital (FMO) analysis were also carried out. Further molecular docking methods were used to recognise the binding of the molecules towards the molecular target DNA (PDB ID: 1BNA), BSA (PDB ID: 3V03) and human aromatase enzyme (PDB-ID: 3EQM). All compounds were screened for their cytotoxicity against breast cancer cell lines (MCF-7) and lung cancer cell lines (A549) under in vitro conditions. The compound 3 showed overall good cytotoxic activity and especially towards MCF-7 (IC50 = 48.5 μM). AO/EB and Hoechst 33258 staining methods were used to analyse morphological changes to expose the mechanism of cell death.

ANTIOXIDANT AND CYTOTOXIC ACTIVITY OF COMBINED EXTRACTS PREPARED USING FICUS RELIGIOSA AND FICUS BENGHALENSIS LEAVES AGAINST CERVICAL CANCER CELL LINE (HELA)

Objectives: Medicinal plants and herbs are used in combination in Ayurveda and folklore medicine as they exhibit good cytotoxic activity. In the present study, the antioxidant, phytochemical, and cell proliferation activity of the combined crude methanolic extract of Ficus religiosa and Ficus benghalensis leaves were investigated.Methods: Antioxidant activity was performed by 2, 2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and hydrogen peroxide methods, and the presence of the phytochemicals was screened using the gas chromatography–mass spectrometry. The extract was further evaluated for its cell proliferation activity against cancer cells using the mitochondrial reduction assay. Antioxidant property of the extracts was measured using the DPPH, hydrogen peroxide, and ferric-reducing antioxidant power assay, respectively, using the UV spectrophotometer.Results: The combined extract exhibited strong antioxidant potential in DPPH assay by increase in the percentage of inhibition with the increase in concentration. Similarly, the IC50 value of the methanol extract in peroxidase scavenging activity was 49.85 μg/mL comparatively lower than the ascorbic acid used as standard. The phytochemical analysis of the methanol extract showed the presence of nine phytoconstituents, which exhibit antioxidant and anticancer property. Mitochondrial reduction assay performed to evaluate the cell proliferation activity of the combined leave extract showed that increase in the concentration of the extract decreased the cell proliferation in the HeLa cell line.Conclusion: The results of present study show a possible synergistic activity of leaves against human cervical cancer.

SYNTHESIS, SPECTRAL CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL THIAZOLE-OXOINDOLE HYBRID COMPOUNDS AS POTENTIAL ANTICANCER AGENTS

In the present study, a series of thiazole derivatives bearing 5-morpholinosulfonylindole were designed and synthesized through condensation of 5-(morpholinosulfonyl)isatin (1) with some thiazolidinone derivatives as carbon nucleophiles to afford the corresponding arylidene derivatives (2-5, 7, 8). Furthermore, many thiazole derivatives (11-15) were obtained through the reaction of thiosemicarbazone derivative (10) with many reagents such as dimethyl acetelenedicarboxylate, phencylbromide derivatives, chloroacetonitrile, chloroacetylchloride as well as chloroacetanilide. The newly synthesized compounds were characterized based on spectral (FT-IR,1H NMR, 13C NMR, MS) analysis. Cytotoxicity effects of all synthesized products were tested against three cancer cell lines, MCF-7, HepG-2, HCT-116 and they showed moderate to good cytotoxic activity against the three tested cell lines. The study showed that compounds (2a, 12b and 12c) were less or almost equipotent as doxorubicin against the three cell lines HepG-2, HCT-116.

Design, Synthesis, Characterization and Biological Evaluation of Ruthenium Complexes of Flavonethiosemicarbazones as Antiproliferative and Mycobacterial Activities

AbstractThe ruthenium(II) complexes of 3‐hydroxy‐4'‐substituted flavonethiosemicarbazones, (where 4'‐substituents are ‐OCH3 (LB1), ‐Cl (LB2), NMe2 (LB3)) with Ru(bpy)2Cl2 and Ru (phen)2Cl2 (bpy=2, 2′ bipyridine; Phen=1, 10 phenanthroline) viz. [Ru(bpy)2(LB1)]Cl2 (MB1), [Ru(bpy)2(LB2)]Cl2.2H2O, (MB2), [Ru(bpy)2(LB3)]Cl2.H2O (MB3), [Ru(phen)2(LB1)]Cl2.H2O, (MP1), [Ru(phen)2(LB2)]Cl2⋅1.5H2O (MP2), [Ru(phen)2(LB3)]Cl2 (MP3) were synthesized in good yield. All the compounds were characterized by elemental analysis, IR, 1H NMR, UV/Vis spectroscopy and ESI‐MS. The spectral features of the complexes matches well to their corresponding formula. The gas phase molecular structures of all complexes were determined using density functional theory (DFT) calculations. All the compounds were screened on A549 (Human Lung carcinoma) cell line using the MTT cell viability assay. The anti‐mycobacterial drug susceptibility testing (DST) was performed using Resazurin Microtiter plate assay with glycerol as carbon source. The effect of compounds on morphological changes of cultured cells was analysed. The compound MB2 showed good cytotoxic activity against human lung carcinoma cell line A549. Similarly, compound MP2 showed good anti‐mycobacterial activity with more than 40% inhibition of growth.

Synthesis of novel guttiferone E and xanthochymol derivatives with cytotoxicities by inducing cell apoptosis and arresting the cell cycle phase

The mixture of GX (guttiferone E and xanthochymol), an inseparable polycyclic polyprenylated acylphloroglucinol (PPAP), showed moderate cytotoxic activities. The chemical transformation of GX yielded three different types of PPAPs (1, 2, and 3/4). A series of analogs were prepared, and the structures of the 40 newly synthesized compounds were elucidated by 1D and 2D NMR and HR-ESI-MS. The derivatives were screened in vitro for antiproliferative activity against five human cancer cell lines: human leukemic cell lines (HEL and K562), cervical cancer cell line (Hela), human breast adenocarcinoma cell line (MCF-7), and human non-small cell lung cancer cell line (A549), using the MTT assay, and most of the derivatives showed good cytotoxic activities. Noticeably, compound 2, a novel tautomer with a hemiketal, exhibited selective cytotoxic activities against HEL (IC50 = 4.79 ± 0.23 μM) and K562 (IC50 = 7.69 ± 0.34 μM) leukemia cells. The mechanism studies indicated that compound 2 induced apoptosis and arrested the cell cycle at the G0/G1 phase in the HEL cell line. Furthermore, compound 2 activated the intrinsic pathway by reducing the expression of anti-apoptotic protein Bcl-2 and cell cycle-specific cyclin D1 and by enhancing the pro-apoptotic protein Bax. Moreover, the caspase-3 and PPRP1 levels were also upregulated. Our present results suggest that compound 2 is a potential candidate for developing novel anti-leukemia agents in the future.