Platinum(IV) combo prodrugs containing cyclohexane-1R,2R-diamine, valproic acid, and perillic acid as a multiaction chemotherapeutic platform for colon cancer.

The complex [PtCl2(cyclohexane-1R,2R-diamine)] has been combined in a Pt(IV) molecule with two different bioactive molecules (i.e., the histone deacetylase inhibitor 2-propylpentanoic acid or valproic acid, VPA, and the potential antimetastatic molecule 4-isopropenylcyclohexene-1-carboxylic acid or perillic acid, PA) in order to obtain a set of multiaction or multitarget antiproliferative agents. In addition to traditional thermal synthetic procedures, microwave-assisted heating was used to speed up their preparation. All Pt(IV) complexes showed antiproliferative activity on four human colon cancer cell lines (namely HCT116, HCT8, RKO and HT29) in the nanomolar range, considerably better than those of [PtCl2(cyclohexane-1R,2R-diamine)], VPA, PA, and the reference drug oxaliplatin. The synthesized complexes showed pro-apoptotic and pro-necrotic effects and the ability to induce cell cycle alterations. Moreover, the downregulation of histone deacetylase activity, leading to an increase in histone H3 and H4 levels, and the antimigratory activity, indicated by the reduction of the levels of matrix metalloproteinases MMP2 and MMP9, demonstrated the multiaction nature of the complexes, which showed biological properties similar to or better than those of VPA and PA, but at lower concentrations, probably due to the lipophilicity of the combo molecule that increases the intracellular concentration of the single components (i.e., [PtCl2(cyclohexane-1R,2R-diamine)], VPA and PA).

A Conformationally Restricted Gold(III) Complex Elicits Antiproliferative Activity in Cancer Cells.

Diamine ligands are effective structural scaffolds for tuning the reactivity of transition-metal complexes for catalytic, materials, and phosphorescent applications and have been leveraged for biological use. In this work, we report the synthesis and characterization of a novel class of cyclometalated [C^N] Au(III) complexes bearing secondary diamines including a norbornane backbone, (2R,3S)-N2,N3-dibenzylbicyclo[2.2.1]heptane-2,3-diamine, or a cyclohexane backbone, (1R,2R)-N1,N2-dibenzylcyclohexane-1,2-diamine. X-ray crystallography confirms the square-planar geometry and chirality at nitrogen. The electronic character of the conformationally restricted norbornane backbone influences the electrochemical behavior with redox potentials of -0.8 to -1.1 V, atypical for Au(III) complexes. These compounds demonstrate promising anticancer activity, particularly, complex 1, which bears a benzylpyridine organogold framework, and supported by the bicyclic conformationally restricted diaminonorbornane, shows good potency in A2780 cells. We further show that a cellular response to 1 evokes reactive oxygen species (ROS) production and does not induce mitochondrial dysfunction. This class of complexes provides significant stability and reactivity for different applications in protein modification, catalysis, and therapeutics.

The new quinazoline derivative (N2-methyl-N4-[(thiophen-2-yl)methyl]quinazoline-2,4-diamine) vasodilates isolated mesenteric arteries through endothelium-independent mechanisms and has acute hypotensive effects in Wistar rats.

During the screening of new N2,N4-disubstituted quinazoline 2,4-diamines as phosphodiesterase-5 inhibitors and pulmonary artery vasodilators, one N2-methyl-N4-[(thiophen-2-yl)methyl]quinazoline-2,4-diamine (compound 8) presented a greater selectivity for systemic than pulmonary vasculature. The present study aimed to characterize its vasorelaxant and hypotensive effects in Wistar rats. Vasorelaxant effects of compound 8 and underlying mechanisms were evaluated on isolated mesenteric arteries. Acute hypotensive effect was evaluated in anesthetized rats. Additionally, cell viability and cytochrome P450 (CYP) activities were studied in rat isolated hepatocytes. Nifedipine was used as a comparator. Compound 8 induced a strong vasorelaxant effect, similar to nifedipine. This was unaffected by endothelium removal but was decreased by inhibitors of guanylate cyclase (ODQ) and KCa channel (iberiotoxin). Compound 8 enhanced sodium nitroprusside-induced relaxation, but inhibited vasoconstriction evoked by α1-adrenergic receptor activation and extracellular Ca2+ influx via receptor-operated Ca2+ channels. Acute intravenous infusion of compound 8 (0.05 and 0.1 mg/kg) produced hypotension. It showed similar potency to nifedipine for lowering diastolic and mean arterial blood pressure, but less so for the effect on systolic blood pressure. Compound 8 had no effect on hepatocyte viability and CYP activities except at high concentration (10 µM) at which a weak inhibitory effect on CYP1A and 3A was observed. In conclusion, this study identified a N2-methyl-N4-[(thiophen-2-yl)methyl]quinazoline-2,4-diamine with a potent vasodilator effect on resistance vessels, leading to an acute hypotensive effect and a low risk of liver toxicity or drug-drug interactions. These vascular effects were mediated mainly through sGC/cGMP pathway, opening of KCa channels, and inhibition of calcium entry.

Chiral 8-Amino-5,6,7,8-tetrahydroquinoline Derivatives in Metal Catalysts for the Asymmetric Transfer Hydrogenation of 1-Aryl Substituted-3,4-dihydroisoquinolines as Alkaloids Precursors.

Chiral diamines based on an 8-amino-5,6,7,8-tetrahydroquinoline backbone, known as CAMPY (L1), or the 2-methyl substituted analogue Me-CAMPY (L2) were employed as novel ligands in Cp* metal complexes for the ATH of a series of substituted dihydroisoquinolines (DHIQs), known for being key intermediates in the synthesis of biologically active alkaloids. Different metal-based complexes were evaluated in this kind of reaction, rhodium catalysts, C3 and C4, proving most effective both in terms of reactivity and enantioselectivity. Although modest enantiomeric excess values were obtained (up to 69% ee in the case of substrate I), a satisfactory quantitative conversion was successfully fulfilled even in the case of the most demanding hindered substrates when La(OTf)3 was used as beneficial additive, opening up the possibility for a rational design of novel chiral catalysts alternatives to the Noyori-Ikariya (arene)Ru(II)/TsDPEN catalyst.

Structural, vibrational spectroscopy, molecular docking, DFT studies and antibacterial activity of (E)-N1-(3-chlorobenzylidene)benzene-1,4-diamine.

In this work, (E)-N1-(3-chlorobenzylidene)benzene-1,4-diamine (CBD) compound was synthesized with good yield. The spectral studies were recorded by FT-IR, FT-Raman, NMR and UV-Vis to determine structural parameters. The geometrical parameters were optimized using DFT calculations at 6-311++G(d,p) basis set. The calculated structural parameters of the molecule were in line with the experimental data. The molecular orbitals of the compound were investigated through highest occupied molecular orbital (HOMO), lowest unoccupied molecular orbital (LUMO) analysis. The hyper conjugative interaction energy E(2) along with donor, acceptor electron densities (EDs) were determined by natural bond orbital (NBO) analysis. The molecular electrostatic potential (MEP), mulliken atomic charges, non-linear optical (NLO) properties and potential energy surface (PES) scan were also calculated. The 1H and 13C NMR chemical shifts calculated using Gauge invariant atomic orbital (GIAO) method were compared with the experimental NMR chemical shifts. Thermogravimetry (TG) and Differential Scanning Calorimetry (DSC) were carried out to characterise the thermal behaviour and stability of CBD molecule. In addition, PreADMET tool was also used to estimate ADME and Toxicity of CBD compound. The compound screened against four pathogens two gram positive and two gram negative had shown good anti-bacterial behaviour. The molecular docking studies executed against anti-bacterial target topoisomerase DNA gyrase enzyme (2XCT) emphasized good binding behaviour over the standard drug.Communicated by Ramaswamy H. Sarma.

Electrochemical synthesis of vicinal azidoacetamides.

Vicinal diamines are an important structural motif in bioactive natural products and pharmaceutical intermediates. Herein, an environmentally friendly and efficient electrochemical approach to azidoacetamides, as one variant of vicinal diamines, has been developed. This reaction features mild conditions and broad substrate scope, without the use of any chemical oxidant or transition-metal catalysts. The obtained vicinal azidoacetamides could be conveniently converted into various other vicinal diamine derivatives.

Accelerated synthesis of phthalimide derivatives: Intrinsic reactivity of diamines towards phthalic anhydride evaluated by paper spray ionization mass spectrometry.

RATIONALE: Paper spray (PS) is a simple and innovative ambient ionization technique for mass spectrometry (MS) analysis. Under PS-MS conditions, chemical reactions, which usually occur slowly on a bulk scale, are accelerated. Moreover, the formation of products and transient species can be easily monitored. In this manuscript, reactions between phthalic anhydride and diamines were conducted and monitored using a PS-MS platform. The reaction products (phthalimides) have many pharmaceutical applications, but their traditional syntheses can take hours under reflux, requiring laborious purification steps. METHODS: In situ reactions were performed by dropping methanolic solutions of phthalic anhydride and diamines on a triangular paper. The analyses were achieved by positioning the triangle tip in front of the mass spectrometer entrance, whereas a metal clip was attached to the triangle base. After adding methanol to the paper, a high voltage was applied across the metal clip, and the mass spectra were acquired. RESULTS: The intrinsic reactivity of alkyl and aromatic diamines was evaluated. The carbon chain remarkably influenced the reactivity of aliphatic diamines. For aryl diamines, the ortho isomer was the most reactive. Moreover, for aryl amines with electron-withdrawing substituents, no reaction was noticed. CONCLUSIONS: Taking advantage of the unique characteristics of PS-MS, it was possible to investigate the intrinsic reactivity of model alkyl (ethylene versus propylene) and aryl (o-phenylene versus m-phenylene and p-phenylene) diamines towards phthalic anhydride. Some crucial parameters that affect the intrinsic reactivity of organic molecules, such as isomerism, intramolecular interaction, and conformation, were easily explored.

Molecular Design, Preparation, and Characterization of Fluoro-Containing Polyimide Ultrafine Fibrous Membranes with High Whiteness, High Thermal Stability, and Good Hydrophobicity.

Polymeric ultrafine fibrous membranes (UFMs) with high thermal stability and high whiteness are highly desired in modern optoelectronic applications. A series of fluoro-containing polyimide (FPI) UFMs with high whiteness, good thermal stability, and good hydrophobicity were prepared via a one-step electrospinning procedure from the organo-soluble FPI resins derived from a fluoro-containing dianhydride, 4,4'-(hexafluoroisopropylidene) diphthalic anhydride (6FDA), and various diamines containing either pendant trifluoromethyl (-CF3) groups or alicyclic units in the side chains. The obtained FPI UFMs, including FPI-1 from 6FDA and 3,5-diaminobenzotrifluoride (TFMDA), FPI-2 from 6FDA and 2'-trifluoromethyl-3,4'-oxydianiline (3FODA), FPI-3 from 6FDA and 1,4-bis[(4-amino-2-trifluoromethyl)phenoxy]benzene (6FAPB), FPI-4 from 4,4'-bis[(4-amino-2-trifluoromethyl)phenoxy]biphenyl (6FBAB), and FPI-5 from 6FDA and 4'-tert-butyl-cyclohexyl-3,5-diaminobenzoate (DABC) showed whiteness indices (WI) higher than 87.00 and optical reflectance values higher than 80% at the wavelength of 457 nm (R457), respectively. The FPI-5 UFM, especially, showed the highest WI of 92.88. Meanwhile, the prepared PI UFMs exhibited good hydrophobic features with water contact angles (WCA) higher than 105°. At last, the PI UFMs exhibited good thermal stability with glass transition temperatures (Tg) higher than 255 °C, and the 5% weight-loss temperatures (T5%) higher than 510 °C in nitrogen.

A closer look at N2,6-substituted 1,3,5-triazine-2,4-diamines: Advances in synthesis and biological activities.

N2,6-Substituted 1,3,5-triazine-2,4-diamines (N2-substituted guanamines) attracted significant interest due to their potential in the development of bioactive molecules. With just two points of diversity, this scaffold is proved to be suitable for constructing compounds targeting various enzymes, receptors, transporters, and nucleic acids with an array of therapeutic applications, particularly in cancer, inflammation, and CNS disorders. This review discusses progress in the synthesis of N2,6-substituted 1,3,5-triazine-2,4-diamines and their biological activities ranging from the inhibition of cancer-related enzymes (e.g. DNA topoisomerase IIα, carbonic anhydrases, ubiquitin-conjugating enzyme 2B, lysophosphatidic acid acyltransferase ß and various kinases) to the binding to CNS-relevant receptors (e.g. histamine H4, serotonin 5-HT6, adenosine A2a, and α7 nicotinic acetylcholine receptors).

Conformational enantiodiscrimination for asymmetric construction of atropisomers.

Molecular conformations induced by the rotation about single bonds play a crucial role in chemical transformations. Revealing the relationship between the conformations of chiral catalysts and the enantiodiscrimination is a formidable challenge due to the great difficulty in isolating the conformers. Herein, we report a chiral catalytic system composed of an achiral catalytically active unit and an axially chiral 1,1'-bi-2-naphthol (BINOL) unit which are connected via a C-O single bond. The two conformers of the catalyst induced by the rotation about the C-O bond, are determined via single-crystal X-ray diffraction and found to respectively lead to the formation of highly important axially chiral 1,1'-binaphthyl-2,2'-diamine (BINAM) and 2-amino-2'-hydroxy-1,1'-binaphthyl (NOBIN) derivatives in high yields (up to 98%), with excellent enantioselectivities (up to 98:2 e.r.) and opposite absolute configurations. The results highlight the importance of conformational dynamics of chiral catalysts in asymmetric catalysis.

Synthesis of 1,2-Diamines from Vinyl Sulfonium Salts and Arylamines.

A procedure for the synthesis of 1,2-diamines from vinyl sulfonium salts and arylamines under mild conditions was developed. This present synthetic protocol not only obviates the need for a transition-metal catalyst and an oxidizing reagent but also features a broad substrates scope. The practicability of this protocol is demonstrated by the one-pot synthesis, a scale-up reaction, and transformations of the products to diverse N-heterocyclic compounds. Mechanistic studies indicate that the formation of aziridine plays a key role during this diamination process.

Natural Product-Inspired Chiral Ligand Design: Aloperine and N-Substituted Aloperines-Induced Pd-Catalyzed Asymmetric Hydroarylation of Ketimines.

A naturally occurring alkaloid aloperine was utilized as a chiral skeleton for the development of new ligands/catalysts in asymmetric synthesis. A number of N-substituted aloperines have been prepared, and a Pd-catalyzed asymmetric hydroarylation of ketimines using these chiral 1,3-diamine ligands was reported. A range of chiral sulfonyl amides were prepared in high yields and enantioselectivities. The stereoselectivity and structure relationships of aloperines have been studied. In addition, preliminary studies on the desymmetrization of meso-anhydride have also shown that these diamines have good potential in organocatalysis. These discoveries would provide a new future development for natural product-inspired chiral ligand design and developments.

Potential Building Blocks for 1,4-Dihydro-N-heteroacenes.

Studies have been performed aimed at the synthesis of N-heteroacenes via substitution reactions of 4,5-difluoro-1,2-dinitrobenzene with a diamine. The fluorine atoms are displaced first, followed by an activated nitro group. Two intermediates have been characterised by X-ray single-crystal structure determinations. Their intermolecular interactions were examined by Hirshfeld surfaces to assess their suitability for organic molecular electronics. The high reactivity of the phenazine, which is prone to oxidise and rearrange, as are displacement products prepared from it, is explained by the formation of a cis-aci-nitro form from the secondary amine of the phenazine and a nitro group.

Functionalization of Diamine-Appended MOF-Based Adsorbents by Ring Opening of Epoxide: Long-Term Stability and CO2 Recyclability under Humid Conditions.

Although diamine-appended metal-organic framework (MOF) adsorbents exhibit excellent CO2 adsorption performance, a continuous decrease in long-term capacity during repeated wet cycles remains a formidable challenge for practical applications. Herein, we present the fabrication of diamine-appended Mg2(dobpdc)-alumina beads (een-MOF/Al-Si-Cx; een = N-ethylethylenediamine; x = number of carbon atoms attached to epoxide) coated with hydrophobic silanes and alkyl epoxides. The reaction of epoxides with diamines in the portal of the pore afforded sufficient hydrophobicity, hindered the penetration of water vapor into the pores, and rendered the modified diamines less volatile. een-MOF/Al-Si-C17-200 (een-MOF/Al-Si-C17-y; y = 50, 100, and 200, denoting wt % of C17 with respect to the bead, respectively), with substantial hydrophobicity, showed a significant uptake of 2.82 mmol g-1 at 40 °C and 15% CO2, relevant to flue gas concentration, and a reduced water adsorption. The modified beads maintained a high CO2 capacity for over 100 temperature-swing adsorption cycles in the presence of 5% H2O and retained CO2 separation performance in breakthrough tests under humid conditions. This result demonstrates that the epoxide coating provides a facile and effective method for developing promising adsorbents with high CO2 adsorption capacity and long-term durability, which is a required property for postcombustion applications.

Cu-Electrocatalytic Diazidation of Alkenes at ppm Catalyst Loading.

The 1,2-diamine motif is prevalent in natural products, small-molecule pharmaceuticals, and catalysts for asymmetric synthesis. Transition metal catalyzed alkene diazidation has evolved to be an attractive strategy to access vicinal primary diamines but remains challenging, especially for practical applications, due to the restriction to a certain type of olefins, the frequent use of chemical oxidants, and the requirement for high loadings of metal catalysts (1 mol % or above). Herein we report a scalable Cu-electrocatalytic alkene diazidation reaction with 0.02 mol % (200 ppm) of copper(II) acetylacetonate as the precatalyst without exogenous ligands. In addition to its use of low catalyst loading, the electrocatalytic method is scalable, compatible with a broad range of functional groups, and applicable to the diazidation of α,ß-unsaturated carbonyl compounds and mono-, di-, tri-, and tetrasubstituted unactivated alkenes.

Enantio- and Regioselective Construction of 1,4-Diamines via Cascade Hydroamination of Methylene Cyclopropanes.

Despite the widespread existence of chiral 1,4-diamines in bioactive molecules and their applications in asymmetric catalysis, the catalytic and asymmetric synthesis of such structures from readily accessible substrates remains a long-standing challenge. Here, we report a Cu-catalyzed asymmetric cascade hydroamination protocol to construct a wide range of chiral 1,4-diamine derivatives in high yields with excellent enatioselectivities (up to 95 % yield and up to >99 % ee). The use of two hydroxylamine esters containing different functionalized amino groups allowed us to increase the complexity of the final 1,4-diamine structures. The desired products could be easily transformed into chiral 1,4-diamines and chiral NH2 -Terfenadine. Mechanistic study demonstrates that this reaction proceeds through hydroamination ring-opening and cascade hydroamination sequence.

Histological and histochemical characteristics of lacrimal glands in beluga whales (Delphinapterus leucas).

The objective of this study was to describe the histological and histochemical characteristics of the lacrimal glands of beluga whales. The study was carried out on the formalin-fixed ocular globes from 96 carcasses of beluga whales found stranded in the St. Lawrence estuary in Quebec, Canada. Hematoxylin and eosin (H&E) stained slides from the eyes of each whale were examined for lacrimal glands. Histological description was done with H&E and Masson Trichrome (MT) stains. Period Acid-Schiff (PAS), Alcian blue (AB) pH 1.0 and 2.5, and High Iron Diamine (HID) stains were used for histochemical characterization of glycoproteins. Thirteen ocular samples from animals ranging from neonate to 48 y included sections of lacrimal glands. The H&E stain revealed a tubuloalveolar gland architecture, separated into lobules by dense connective tissue. Each lobule contained a mixture of acini and tubules with ductules. Small and large acini were composed of low and tall columnar cells, respectively. Acinar cells contained basophilic cytoplasmic granules. The ductules were lined with a bi-layered cuboidal-to-squamous epithelium. The MT stain highlighted the connective tissue separating ductules and acini. Large acini were positive for PAS and some small acini had patchy uptake. Positive staining for AB pH 1.0 and 2.5 was mainly seen in tall columnar cells as compared to small acini that had faint to no stain uptake. High Iron Diamine stain revealed 90% staining of all acinar cells, with 10% exhibiting a mixed blue-black tinge. It was concluded that the lacrimal glands of beluga whales have similar histological and histochemical findings to those of artiodactyla and carnivora orders.

L'objectif de cette étude était de décrire les caractéristiques histologiques et histochimiques des glandes lacrymales des bélugas. L'étude a été réalisée sur les globes oculaires fixés au formol de 96 carcasses de bélugas trouvées échouées dans l'estuaire du Saint-Laurent au Québec, Canada. Des lames colorées à l'hématoxyline et à l'éosine (H&E) des yeux de chaque baleine ont été examinées pour la présence de glandes lacrymales. La description histologique a été réalisée avec des colorations H&E et trichrome de Masson (MT). Les colorations Periodic acid-Schiff (PAS), au bleu Alcian (AB) pH 1,0 et 2,5, et diamine à haute teneur en fer (HID) ont été utilisées pour la caractérisation histochimique des glycoprotéines. Treize échantillons oculaires provenant d'animaux allant du nouveau-né à 48 ans comprenaient des sections de glandes lacrymales. La coloration H&E a révélé une architecture de glande tubulo-alvéolaire, séparée en lobules par un tissu conjonctif dense. Chaque lobule contenait un mélange d'acini et de tubules avec des ductules. Les petits et les grands acini étaient respectivement composés de cellules cylindriques basses et hautes. Les cellules acinaires contenaient des granules cytoplasmiques basophiles. Les canaux étaient tapissés d'un épithélium cuboïde à squameux bicouche. La coloration MT a mis en évidence le tissu conjonctif séparant les canaux et les acini. Les grands acini étaient positifs pour le PAS et certains petits acini avaient une absorption inégale. Une coloration positive pour AB pH 1,0 et 2,5 a été principalement observée dans les cellules cylindriques hautes par rapport aux petits acini qui avaient une absorption de coloration faible ou nulle. La coloration HDI a révélé une coloration de 90 % de toutes les cellules acinaires, 10 % présentant une teinte mixte bleu-noir. Il a été conclu que les glandes lacrymales des bélugas présentent des résultats histologiques et histochimiques similaires à ceux des ordres des artiodactyles et des carnivores.(Traduit par Docteur Serge Messier).

Discovery and optimization of cyclohexane-1,4-diamines as allosteric MALT1 inhibitors.

Inhibition of mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) is a promising strategy to modulate NF-κB signaling, with the potential to treat B-cell lymphoma and autoimmune diseases. We describe the discovery and optimization of (1s,4s)-N,N'-diaryl cyclohexane-1,4-diamines, a novel series of allosteric MALT1 inhibitors, resulting in compound 8 with single digit micromolar cell potency. X-ray analysis confirms that this compound binds to an induced allosteric site in MALT1. Compound 8 is highly selective and has an excellent in vivo rat PK profile with low clearance and high oral bioavailability, making it a promising lead for further optimization.

Efficacy of 30% and 38% Silver Diamine Fluoride in Arresting Caries Lesions After Different Application Times: An in Vitro Study

Abstract Objective: To evaluate the efficacy of silver diamine fluoride (SDF) in arresting dentin caries lesions when applied under different concentrations and times. Material and Methods: Forty-two bovine blocks were selected and fixed in 24-well plates. Each well received a mixed bacterial inoculum added to the culture medium with 5% sucrose. The plates were incubated in microaerophilia (7 days) for caries formation, confirmed by micro-CT (M1). SDF was applied over the carious lesions for different times and concentrations (n=6): SDF 30% - immediate removal, 1 minute and 3 minutes; SDF 38%, - immediate removal, 1 minute and 3 minutes. The group without treatment was the control. Then, the samples were again scanned by micro-CT (M2) and submitted to a second cariogenic challenge for 21 days. Then, a final scan was performed (M3). Results: Mean pH at the culture medium and lesion depth were compared using Kruskal-Wallis and Wilcoxon tests. 38% SDF showed the lowest metabolic activity of the biofilm. All 38% groups and 30% 1 and 3 minutes did not show an increase in mean lesion depth comparing M3 with M1. However, only 30% 3 minutes and 38% 1 and 3 minutes showed a significant reduction of lesion depth. Conclusion: The minimum application time of 30% SDF to arrest dentin caries lesion was 1 minute, while 38% SDF arrested with application and immediate removal.

Bivalent ß-Carbolines Inhibit Colorectal Cancer Growth through Inducing Autophagy.

In this study, a series of alkyl diamine linked bivalent ß-carbolines was synthesized and evaluated as antitumor agent. The results demonstrated that most compounds displayed good antiproliferative activities with IC50 value lower than 10 µM against a panel of human tumor cell lines, and compound 8 was found to be the most potent antiproliferative agent with IC50 value of 1.39, 1.96, 1.42, 1.49, 1.32, 1.96 and 1.63 µM against human breast cancer cell line (MCF-7), human adenocarcinoma cell line (769-P), human malighant melanoma cell line (A375), human ovarian cancer cell line (SK-OV-3), human colon carcinoma cell line (HCT-116), human gastric cancer cell line (BGC-823) and human esophageal squamous carcinoma cell line (Eca-109), respectively. Further investigations on mechanism of action of this class of compound demonstrated that the representative compound 8 inhibited colorectal cancer growth through inducing autophagy.