Synthesis, Characterization and Cytotoxicity of Ammine/Methylamine Platinum(Ⅱ) Complexes with Carboxylates

Seven novel platinum (Ⅱ) complexes [Pt (Ⅱ) (NH3) (CH3NH2) X2] (Ⅰ -Ⅶ) (X: CH3COO- ,CH2 ClCOO - , CHCl2COO -, C6H5-COO - , p-CH3O-C6H4 -COO - , p-NH2-C6 H4 -COO - , p-NO2 -C6 H4 -COO-) were prepared and characterized by means of elemental analysis, molar conductivity, thermal analysis,IR, UV, and 1 H NMR spectrometries. The cytotoxicity against HCT-8, BGC-823, MCF-7, EJ, and HL-60 cell lines increases in the following sequence: cisplatin ＞Ⅳ＞Ⅴ＞Ⅵ＞Ⅶ＞Ⅰ＞Ⅱ＞Ⅲ. Moreover, the complexes(Ⅰ -Ⅶ) display substantially greater activities against EJ and HL-60 cell lines than those against the cell lines from other carcinomas. They can induce a concentration-dependent accumulation of HL-60 cells in the G2/M phase of the cell cycle as cisplatin. There is no significant correlation between total DNA platination levels and cytotoxicity of the complexes.     

Synthesis and cytotoxicity evaluation of a novel justicidin G analogue and its phosphate ester

The novel justicidin G analogue 13 and its phosphate ester 15 were synthesized as potential anticancer agents in several steps starting from commercially available methyl gallate and veratraldehyde. The cytotoxicity of the intermediates was tested against HCT-8, BEL-7402, KETR3, HELA, BGC-823, KB and MCF-7 cell lines by the MTT test, and compound 15 exhibited significant cytotoxicity in HELA and KB cell lines.     

新型铂(Ⅱ)类配合物的合成、表征和抗肿瘤活性

Seven novel platinum(Ⅱ) complexes[Pt(Ⅱ)(NH₃)(H₂O)X](Ⅰ～Ⅶ) {X=(COO^-)₂(oxalato), 2p-CH₃O-C₆H₄-COO^-(p-methyoxbenzolato), 2C₆H₅-COO^-(benzolato), 2CH₃COO^-(acetato), (CH₂)(COO^-)₂(malonato), (CH₂)₂(COO^-)₂(succinato), (CH=CH)(COO^-)₂(maleato)} have been prepared and characterized by elemental analysis, thermal analysis，IR, UV, and ¹H NMR spectroscopy. The antitumor activities of these complexes in vitro against EJ、HCT-8, KB, BGC-823, Bel-7402, HL-60, MCF-7 and Hela cell lines have been studied. Complex Ⅰ and Ⅴ show remarkable antitumor activities against EJ cell line, and the inhibitory rate is 45.96% and 54.32% at concentration of 10 μmol·L^-1, respectively. The inhibitory rate of the complexes Ⅱ and Ⅲ is greater than 50% against HL-60, BGC-823, KB and EJ cell lines. The inhibitory rate of the complex Ⅵ is 51.89% and 57.96% against BGC-823 and EJ cell lines. The complexes Ⅳ and Ⅶ have no antitumor activities against tested tumor cell lines. The complexes Ⅱ, Ⅲ and Ⅵ can stem the cell cycle of HL-60 on the G₂+M.     

Synthesis, characterization, crystal structure and antitumor activities of a novel demethylcantharidato bridged copper(II) phenanthroline complex

A new polymeric demethylcantharidato (DCA) bridged copper(Ⅱ) phenanthroline (phen) complex ([Cu(DCA)(phen)] n ·nH2O) has been synthesized and characterized by elemental analysis, IR and electronic spectra studies, molar conductivity measurement, and single crystal X-ray diffraction. The complex crystallizes in the orthorhombic space group Pbca with crystallographic data: a = 12.4537(4), b = 9.3897(5), c = 30.1264(10), and Z = 8. In the crystal structure, the octahedral coordinated copper(Ⅱ) ions are bridged by demethylcantharidate ligands into a one-dimensional zigzag-like structure with the Cu···Cu separation of 6.1719, along with phen ligands attached to both sides of the chain alternatively. Interdigitation of the chelating phen ligands of two neighboring chains via hydrophobic interaction and van der Waals forces along ac plane forms two-dimensional polymeric bilayers with discrete water sandwich layer between the adjacent polymeric bilayers. The evaluation of the cytotoxic activity of the copper(Ⅱ) complex against HCT-8 (colorectal carcinoma), A549 (pulmonary carcinoma), HeLa (cervical cancer), HepG2 (hepatocarcinoma), BGC-823 (gastric carcinoma), and MCF-7 (breast adenocarcinoma) cell lines revealed that it is a potent cytotoxic agent, superior to Na2DCA and phen against HeLa, HepG2 and BGC-823 cells.     

Synthesis and in vitro cytotoxicity of novel 1,4-disubstituted phthalazines

Eight novel 1,4-disubstituted phthalazines （7-14） were designed and synthesized. The structures of all the synthesized compounds were confirmed by IR,1H NMR, 13C NMR, MS and elemental analysis. Their in vitro cytotoxicity against cancer cell lines （Bel-7402 and HT- 1080） were evaluated by standard MTT assay. Among them, compounds 9 and 11 exhibited more potent cytotoxicity than cisplatin. 2007 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.     

Synthesis,Crystal Structure and Antitumor Activities of N,N,1-Triphenyl-1H-benzo[d]imidazol-5-amine Derivatives

In order to discover the novel antitumor agents, a series of N,N,1-triphenyl-~1Hbenzo[d]imidazol-5-amine derivatives were designed and synthesized, and the structures were characterized by IR, H-RMS, ~1H and ~(13)C NMR. X-ray crystallography showed that 4 c is in monoclinic system, space group P1 with a = 9.209(2), b = 9.533(3), c = 14.097(3) ?, β = 102.069(3)°, V = 1202.2(5) ?~3, Z = 2, F(000) = 528, μ = 1.74 mm–1, S = 1.024, the final R = 0.0448 and wR = 0.1109. The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer cell lines K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activities against these cell lines.     

芳香亚胺与N-(4-甲基苯甲酰)-L-缬氨酸双阴离子合钯(Ⅱ)配合物的合成、晶体结构及体外抗肿瘤活性

本文首次报道了2个钯(Ⅱ)的配合物[Pd(bipy)(4-CH3Bzval-N,O)](1)和[Pd(phen)(4-CH3Bzval-N,O)](2)(bipy=2,2′-联吡啶,phen=1,10-菲咯啉,4-CH3Bzval-N,O=N-(4-甲基苯甲酰)-L-缬氨酸双阴离子)的合成及晶体结构,利用MTT法和SRB法研究了配合物的体外抗肿瘤活性。配合物2属单斜晶系P21/n空间群,其中a=1.162 92(8)nm,b=1.074 03(7)nm,c=1.821 14(12)nm,V=2.232 8(3)nm3,Z=4。结果显示:2个配合物对HL-60,BGC-823,Bel-7402和KB 4种人的肿瘤细胞表现出一定的活性和选择性,但其活性均小于顺铂。     

Two New Compounds from Goniothalamus Cheliensis Hu

Goniothalamus cheliensis Hu (Annonaceace) is a small tree or shrub in Yunnan Province, southwest of China. Acetogenins, styryllactones and alkaloids1-3 from the genus were reported in the previous literature and many of them showed strong cytotoxic activities against a number of human cancer cell lines4. The titled plant has been the subject of our investigation due to the impressive cytotoxicity of its organic extract against mouse lymphocytic leukemia cells in preliminary pharmacological s…     

Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

<正>A series of 2-amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl substituted diaryl urea derivatives was designed and synthesized.Their in vitro cytotoxicities against two cancer cell lines(Bel-7402 and A549) were evaluated by standard MTT assay.Six of tested compounds 6,8,10,17,21 and 22 exhibited more potent cytotoxicity superior to sorafenib.The structure activity relationship(SAR) study indicates that 2-amino-5,6,7,8-tetrahydropyrido- [4,3-d]pyrimidinyl group was an option for cytotoxic potency.     

二维网状Pd(Ⅱ)配合物的合成、晶体结构及电化学性质(英文)

A novel palladium(Ⅱ) complex [Pd(H2bpdc)Ala]Cl·3H2O (where H2bpdc is 2,2′-bipyridine-3,3′-dicar- boxylic acid and Ala is L-alanine) has been synthesized and characterized by IR spectra and elemental analysis. The crystal structure of the complex has been determined by single-crystal X-ray diffraction analysis. It crystallizes in triclinic system, space group P1 with a=0.685 5(2) nm, b=0.988 4(4) nm, c=1.349 6(4) nm, α=98.375(8)°, β= 97.900(15)°, γ=90.118(15)°, V=0.895 9(5) nm3, Z=2. In the molecule, Pd(Ⅱ) atom is four-coordinated and located at the centre of a planar quadrangle. The complex is assembled via intramolecular π-π stacking interactions and hydrogen bonds, which forms 2D network. The cyclic voltammetric behavior of the complex was also investigated.     

三核镍配合物Ni_3(C_(14)H_8N_3O_5)_2(C_5H_5N)_4的合成、晶体结构和抗癌活性(英文)

The title complex Ni3(C14H8N3O5)2(C5H5N)4 has been synthesized by the reaction of 2-hydroxy-N′-(4- nitrobenzoyl)benzohydraizide with nickel acetate in pyridine solution. Its molecular structure was characterized by elemental analysis, IR spectra and X-ray crystal structure determination. Crystal data for this compound: Mono- clinic, space group P21/c, Mr=1 089.00, a=0.249 27(5) nm, b=0.161 40(3) nm, c=0.121 81(2) nm, β=94.59(3)°, V= 4.885 2(17) nm3, Z=4, Dc=1.481 Mg·m-3, F(000)=2 232, R1=0.049 7, wR2=0.106 8 (observed reflections with I2σ(I)) and R1=0.105 1, wR2=0.119 4 (all reflections), GOF=1.021. The complex was evaluated for their antitumor activi- ties against two kinds of cell lines (K562 and BGC) by MTT method. A preliminary bioactivity study indicates that the complex shows distinct antitumor activity.     

Synthesis and crystal structure of a novel two-dimensional network complex [Mn(O_2CCH_2Cl)_2(phen)]_n

A novel two-dimensional network manganese(Ⅱ) polymer complex [Mn(O2CCH2CI)2-(phen)]n has been synthesized and characterized by elemental analysis and IR spectrum. The crystal structure of title complex has also been determined, which is in monoclinic of a space group P21/c with the following unit cell parameters at 294K: a =1.9738(4) nm, b =1.1384(2) nm, c =0.74915(14) nm, V=1.6795(5) nm3, Z= 2.     

Synthesis and antitumor activity of some new pyrazolo[1,5-α]pyrimidines

New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal carcinoma(HCT116),prostate adenocarcinoma(PC-3) and liver carcinoma(HepG-2) using MTT cytotoxicity assay at 100 μg/mL.Some of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 cells.Whereas,compounds 7d and 11 a showed better antitumor activity than the rest of the compounds against both cell lines.A structure-activity relationship(SAR) has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data(MS,IR,~1H NMR and ~(13)C NMR) and elemental analysis.     

Uncinatic acids A-C,three new carboxylated flavonoids from Selaginella uncinata

Three new carboxylated flavonoids, uncinatic acids A-C(1–3), were isolated from the whole herb of Selaginella uncinata. Their structures were established on the basis of extensive NMR analysis including1 D, 2D NMR experiments and HR-ESIMS techniques. All of them share the carboxylation structural characteristic. Compounds 1 and 2 belong to novel naturally occuring furanoflavonoids which is firstly reported in genus Selaginella. Such furanoflavonoids with dicarboxylic acid structrure have never been discovered before. In addition, the isolates were tested for their cytotoxicity against A549 and BGC-823 cell lines in vitro.     

Synthesis,Crystal Structure and in vitro Anticancer Studies of 1,2-Bis-benzimidazole-phenyl Copper(Ⅱ) Complex

One new benzimidazole derivative copper(II) complex 1(C10H6Cu N2, Mr = 217.71) has been synthesized and characterized by FT-IR and X-ray single-crystal diffraction. It crystallizes in orthorhombic, space group Pbcn with a = 17.417(2), b = 8.9963(8), c = 11.3432(9) ?, V = 1777.3(3) ?3, Z = 8, μ(Mo Kα) = 2.403, F(000) = 872, Dc = 1.627 g/cm3. The final R = 0.0598 for 1153 observed reflections with I 2σ(I) and w R = 0.17 for all data. The in vitro anti-cancer activities of 1, Cu Cl2 and the benzimidazole ligand L were investigated using human cervical(Hela) and hepatocellular carcinoma(Hep-G2) cancer cell lines. The copper(II) complex can greatly inhibit the cell proliferation and show stronger cytotoxic activities against the tested cancer cell lines than both the ligand and copper(II) salt.     

Rubratoxin C,a new nonadride derivative from an endophytic fungus Penicillium sp. F-14

One new nonadride derivative rubratoxin C （1） together with a known compound rubratoxin B （2） were isolated from an endophytic fungus Penicillium sp. F-14. Their structures were elucidated by various spectroscopic methods. Bioassays showed that 2 had moderate cytotoxic effect against HCT-8, BEL-7402, Ketr3, A2780, MCF-7 and BGC-823 human cancer cell lines, and 1 exhibited weak activity.     

Synthesis,Crystal Structure and Antitumor Activities of N-(2-(2-hydroxy-2-phenylacetyl)phenyl)cinnamamide

The title compound N-(2-(2-hydroxy-2-phenylacetyl)phenyl)cinnamamide(C_(23)H_(19)NO_3, Mr = 357.39) has been synthesized with 2-iodoaniline and ethynylbenzene as starting materials, and its crystal structure was determined by ~1H NMR, ~(13)C NMR, H RMS and single-crystal X-ray diffraction for the first time. The crystal crystallizes in monoclinic system, space group P21/c with a = 8.2850(7), b = 25.934(2), c = 8.3032(6) ?, β = 95.314(7)°, V = 1776.4(3) ?3, Z = 4, T = 293(2) K, μ(Cu Kα) = 0.71 mm-1, Dc = 1.336 Mg/cm3, 3019 reflections measured(6.832≤2θ≤129.982°), 2996 unique(Rint = 0.0463, Rsigma = 0.0549) which were used in all calculations. The final R = 0.0880(I 2σ(I)) and wR = 0.2447(all data). The target compound has demonstrated weak or moderate anti-tumor activity against human leukemia k562 cell, human promyelocytic leukemia HL-60 cell, human gastric cancer line BGC-823, Hela cell and lung cancer A549 cell.     

Design,synthesis and antitumor activity of 3-substituted quinolone derivatives （Ⅰ）

A series of quinolone derivatives containing benzimidazole, benzoxazole or benzothiazole ring were synthesized. The cytotoxicity of 12 new compounds was evaluated in KB, Be17402, A2780 and HT-29 cell lines. Most of synthesized compounds showed moderate inhibitory activity against cancer cells. The inhibitory activities of 6k, against KB and A2780 tumor ceils are comparable to that of topotecan, one of topoisomerase I inhibitors.     

Synthesis and Cytotoxicity of the First Arene Ruthenium Compound Containing Two Thiosemicarbazone Ligands

A Ru-arene compound containing two thiosemicarbazone ligands [(η6-p-cymene)Ru(TSC)2 Cl]Cl(1, TSC = benzophenone 4-methylthiosemicarbazone) has been synthesized and characterized by 1 H NMR, elemental analysis and HR-ESI mass spectrometry analysis. The molecular structure was determined by single-crystal X-ray diffraction analysis. The in vitro anticancer activities of the complex have been evaluated against two human cancer cell lines(SGC-7901, BEL-7404), and the IC50 values are 32.5 and 57 μM, respectively.     

Synthesis,Crystal Structure and Antitumor Activities of 1,2,3,4-Tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) Derivatives

A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The structures of these derivatives were characterized by H-RMS and NMR analysis. X-ray crystallography showed that 3 a is in a monoclinic system, space group of P2_1/c with a = 13.0464(16), b = 12.6244(16), c = 20.210(3) ?, β = 105.215(2)o, V =3211.9(7) ?~3, Z = 4, F(000) = 1352, μ = 0.42 mm~(–1), S = 1.07, the final R = 0.059 and wR = 0.195.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activity against these cell lines.