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Copper complexes of anthrahydrazone bearing pyridyl side chain:Synthesis,crystal structure,anticancer activity,and DNA binding

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无机化学学报 2025年第1期41卷 213-224页

作者： HUANG Yao WU Yingshu BAO Zhichun HUANG Yue TANG Shangfeng LIU Ruixue LIU Yancheng LIANG Hong School of Chemical Engineering Yunnan Open UniversityKunming 650223China School of Chemistry&Pharmaceutical Sciences Guangxi Normal UniversityGuilinGuangxi 541004China

To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and *** 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination *** chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray *** 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal *** 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper ***,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric *** vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than ***,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell *** addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer ***:

关键词： anthrahydrazone metal complex crystal structure anticancer activity cell apoptosis

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anticancer activity of crude acetone and water extracts of Tulbaghia violacea on human oral cancer cells

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Asian Pacific Journal of Tropical Biomedicine 2018年第9期8卷 456-462页

作者： Samkeliso Takaidza Arumugam Madan Kumar Cornelius Cano Ssemakalu Nagabishek Sirpu Natesh Gayathri Karanam Michael Pillay Department of Biotechnology Vaal University of Technology Cancer Biology Lab Molecular and Nanomedicine Research Unit Sathyabama Institute of Science and Technology

Objective: To evaluate the anticancer activity of crude acetone and water leaf extracts of Tulbaghia violacea on a human oral cancer cell line(KB).Methods: The antioxidant activity of the leaf extracts was evaluated by using the DPPH assay while the anti-proliferative activity was assessed by using the MTT *** morphological characteristics of apoptotic cells were examined by using the dual acridine orange/ethidium bromide *** cytometry was used to evaluate the induction of multi-caspase activity and changes in the cell ***: The acetone and water extracts exhibited antioxidant activity in a concentration dependent *** extracts inhibited the growth of the KB cell line with IC_(50) values of 0.2 mg/mL and 1 mg/mL, respectively for acetone and *** changes such as cell shrinkage, rounding and formation of membrane blebs were observed in the treated *** acridine orange/ethidium bromide staining, the number of apoptotic cells increased as the concentration of the extracts *** activation of multi-caspase activity in KB cells treated with Tulbaghia violacea extracts was concentration dependent, leading to cell death by apoptosis and cell cycle arrest at the G_2/M ***: The acetone and water extracts of Tulbaghia violacea appear to have anti-cancer activity against human oral cancer cells and need to be investigated further.

关键词： anticancer activity Antioxidant Apoptosis Caspase Cell cycle Tulbaghia

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Comparative Molecular Field Analysis(CoMFA) of Curcumin-related Compounds for anticancer activity

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Chinese Journal of Structural Chemistry 2014年第2期33卷 179-188页

作者：周代营杜志云汤志恺郑希丁宁郑俊霞王辉张焜 Allan H. Conney Laboratory for anticancer Research Institute of Natural Medicinal Chemistry & Green Chemistry Guangdong University of Technology Guangdong Food and Drug Vocational College Susan Lehman Cullman Laboratory for Cancer Research Department of Chemical Biology Ernest Mario School of Pharmacy Rutgers The State University of New Jersey Guangzhou Improve Medical Technology Co. Ltd.

Three-dimensional （3D） quantitative structure-activity relationship （QSAR） studies of 44 curcumin-related compounds have been carried out based on our previously reported result for their anticancer activity against pancreas cancer Panc-I cells and colon cancer HT-29 cells. The established 3D-QSAR models from the comparative molecular field analysis （CoMFA） in training set showed not only significant statistical quality, but also satisfying predictive ability, with high correlation coefficient values （R12= 0.911, R22= 0.985） and cross-validation coefficient values （q2= 0.580, q22= 0.722）. Based on the CoMFA contour maps, some key structural factors responsible for anticancer activity of these series of compounds were revealed. The results provide some useful theoretical references for understanding the mechanism of action, designing new curcumin-related compounds with anticancer activity and predicting their activities prior to synthesis.

关键词： curcumin-related compounds QSAR CoMFA anticancer activity Panc-1 HT-29

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Improvement of Stability and anticancer activity of ChlorambuciI-Tetrapeptide Conjugate Vesicles

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Chinese Journal of Chemistry 2016年第6期34卷 609-616页

作者： Wei Zhang Wenjun Zhu Ruiyu He Shuo Fang Yemin Zhang Chen Yao Muhammad Ismail Xinsong Li School of Chemistry and Chemical Engineering Southeast University Nanjing Jiangsu 210096 China

Chlorambucil is a classic nitrogen mustard drug that has been used in the treatment of cancers. It may induce neutropenia, thrombocytopenia and other side effects because of its short lifetime and off-target effect. In this report, chlorambucil-tetrapeptide （AAAK, A3K） conjugate vesicles were developed to improve the stability and bioactivity of chlorambucil. First of all, chlorambucil-A3K conjugate was synthesized by solid phase synthesis strategy. Sec- ondly, the chlorambucil-A3K conjugate was assembled and characterized by critical aggregation concentration, cir- cular dichroism, dynamic light scattering and transmission electron microscopy. The results indicated that the chlo- rambucil-A3K conjugate can be assembled to form spherical vesicles with an average diameter of 390.5 nm, and high drug loading about 47.1% is reached. Surprisingly, the preliminary biological evaluation of the chlorambu- cil-A3K conjugate vesicles revealed the best in vitro anticancer activity against HeLa, HepG-2 and MCF-7 cell lines compared with chlorambucil and chlorambucil-A3K conjugate free drugs. Furthermore, conjugate vesicles showed excellent in vivo antitumoral activity. It can be partly attributed to their vesicular structure which isolates chloram- bucil active moiety from aqueous solution to retard degradation before killing cancer cells. Therefore, chlorambu- cil-peptide （A3K） conjugate vesicles may be an alternative delivery system of chlorambucil.

关键词： chlorambucil-tetrapeptide conjugate self-assembly vesicles anticancer activity

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QSAR Studies on a Series of 7,8-Dialkyl-1,3-diaminopyrrolo-[3,2-f]quinazolines with anticancer activity

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Chinese Journal of Chemistry 2006年第11期24卷 1531-1537页

作者：陈锦灿钱力沈勇陈兰美郑康成 School of Chemistry and Chemical Engineering Zhongshan University Guangzhou Guangdong 510275 China

The quantitative structure-activity relationship （QSAR） studies on a series of 7,8-dialkyl-1,3-diaminopyrrolo-[3,2-f]quinazolines, dihydrofolate reductase （DHFR） inhibitors as potential anticancer agents, have been carried out by using the density functional theory （DFT） method, molecular mechanics method （MM＋） and statistical method. Some QSAR models based on their lipophilic and steric parameters were built up via a stepwise regression analysis. It is very interesting to find that the established optimal QSAR equation involves only two descriptors： lipophilicity indexes Clog P and Clog P^2 However, such descriptors can quite well describe a significant statistic quality and have a remarkable predictive activity according to the square of adjusted correlation coefficient （RA^2 = 0.937） and the square of cross-validation coefficient （q^2=0.911） of this equation. The results show that the lipophilicity is a main factor affecting the anticancer activity of this series of antimetastatic agents, and the obtained equation describes a parabolic correlation between pIC50 and Clog P, and indicates a suitable range of Clog P （around 4.43） being very important for optimal pIC50 values. These QSAR studies can offer some useful references for understanding the action mechanism and performing the molecular design or modification of this series of antimetastatic agents.

关键词： quinazoline anticancer activity density functional theory (DFT) QSAR Clog P

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Potential anticancer activity analysis of piscidin 5-like from Larimichthys crocea

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Acta Oceanologica Sinica 2022年第3期41卷 53-60页

作者： Libing Zheng Jiayin Qiu Huihui Liu Changfeng Chi Longshan Lin National and Provincial Joint Laboratory of Exploration and Utilization of Marine Aquatic Genetic Resources School of Marine Science and TechnologyZhejiang Ocean UniversityZhoushan 316022China Third Institute of Oceanography Ministry of Natural ResourcesXiamen 361005China

Antitumor activity is one characteristic function of some certain antimicrobial peptides(AMPs)found in recent *** the present study,we attempted to detect potential anticancer activity of a recombinant piscidin 5-like from Larimichthys crocea(r Lc-P5L)which owned widely antibacterial and strong antiparasitic activity in *** light microscope observation indicated r Lc-P5L was of antitumor activity to He La cells,293 T cells and L929 *** assay showed the toxic sensitivity of r Lc-P5L to three tumor cell strains was 293 T>L929>He *** electron microscope(SEM)results showed r Lc-P5L behaved like a lytic peptide to cause damage on cells membrane of L929 cells by forming globular clusters,even pores at 60μmol/L,or degrading membrane to make it completely lose cytoskeleton structure at 80μmol/L;r Lc-P5L treatment also resulted in DNA *** observation results indicated r Lc-P5L could cause L929 cells at least two obvious changes:one is nucleus,nuclear chromatin condensed in the margin,nuclear volume became smaller and shrank to be out of shape,or lysed to be debris;the other is cytoskeleton,they became disordered and polarized to make cells atrophic shapes,or even lysed to be *** summary,r Lc-P5L owned potential anticancer activity causing membrane structure damage and genome DNA ***,treatment with different concentration of r Lc-P5L seemingly caused the similar but different changes,whether it indeed gave rise to cancer cells diverse death way,the further studies should be performed,and the detailed mechanisms were still need further explored.

关键词： Larimichthys crocea piscidin 5-like anticancer activity membrane destruction DNA degradation

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Design, Synthesis and anticancer activity of Novel 6-（Aminophenyl）-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety

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Chemical Research in Chinese Universities 2014年第2期30卷 257-265页

作者： HUANG Qiang FU Qiangqiang LIU Yajing BAI Jinying WANG Qianying LIAO Huimin GONG Ping Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationShenyang Pharmaceutical University Shenyang 110016 P.R.China

In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis（morpholino-1,3,5-triazine） derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460（non-small-cell lung cancer）,HT-29（human colorectal cancer） and MDA-MB-231（human breast cancer） cell *** pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds（7e,7h,7j,9a,9b,9c） were superior to PAC-1 against all the tested cancer cell *** most active compound 7j,with IC50（inhibitory concentration 50％）values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 （29.24,9.52 and 36.21 μmol/L）,respectively.

关键词： Bis(morpholino-1,3,5-triazine) Design anticancer activity

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Two Cu(Ⅱ)and Co(Ⅱ)-based Coordination Polymers Based on the N,S-donor Ligand:Crystal Structures and anticancer activity Evaluation

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Chinese Journal of Structural Chemistry 2020年第10期39卷 1849-1854,1744页

作者： LI Jing LI Jiang-Tao Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province School of Chemical EngineeringXi'an UniversityXi'an 710065China

Two new Cu(II)and Co(II)-based coordination polymers with the chemical formulae of{Cu(L)2]·DMF}n(1)and{[Co(L)2]·2DMF}n(2)have been successfully constructed from a pyridine-substituted N-heterocyclic thioamide ligand,namely[3,4?-bipyridine]-2?-thiol(HL).Complex 1 is composed of two identical coordination networks with dia topology interpenetrating into each other,and shows 1-D microporous channels along the a *** 2 is assembled by 2-D square-grid layers stacked in an eclipsed fashion to give 1-D large square channels along the b ***-8 was used for the detection of cancer *** indicated that compound 1 exhibited stronger anti-cancer activity than compound 2 on the H1650 cancer *** Annexin V-FITC/PI was recommended for cancer cell apoptosis,and the western blot was applied for the detection of PI3K/AKT pathway activation.

关键词： coordination polymer N S-donor ligand CCK-8 assay anticancer activity

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Total synthesis and anticancer activity studies of the stereoisomers of asperphenamate and patriscabratine

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Chinese Chemical Letters 2010年第2期21卷 155-158页

作者： Yuan, Lei Wang, Jin Hui Sun, Tie Min Shenyang Pharmaceut Univ Sch Pharmaceut Engn Shenyang 110016 Peoples R China Shenyang Pharmaceut Univ Sch Traditt Chinese Mat Med Shenyang 110016 Peoples R China

All stereoisomers of asperphenamate 1a and patriscabratine 2a were achieved with a high yield,and total synthesis of 2a is firstly described *** absolute configuration of patriscabratine was determined as(S,S).The compounds 1a-d and 2a-d have been tested by MTT assay in T47D,MDA-MB231,HL60,Hela and SGC-7901 cell lines in *** them,the(R,S) stereoisomer shows the strongest anticancer effects,while the(S,R) shows the weakest one.

关键词： N N -substituted phenylalanine-phenylalaninol ester Asperphenamate Patriscabratine Total synthesis anticancer activity

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Facile Synthesis of 7-epi-Taxane and Its Derivatives and Preliminary Evaluation of anticancer activity

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Chinese Journal of Chemistry 2016年第11期34卷 1165-1176页

作者： Zhao Li Jia Feng Kun Zou Zhuo Yang Yong Zhang Zhijian Xu Bo Li Jiye Shi Yiming Li Weiliang Zhu Kaixian Chen School of Pharmacy Shanghai University of Traditional Chinese Medicine Shanghai 201203 China CAS Key Laboratory of Receptor Research Drug Discovery and Design Centre Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China Nano Science and Technology Institute University of Science and Technology of China Suzhou Jiangsu 215123 China UCB Biopharma SPRL Chemin du Foriest Braine-l'Alleud Belgium Kellogg College University of Oxford 60-62 Banbury Road Oxford OX2 6PN United Kingdom

7-epi-Taxane has been achieved efficiently in gram scale from natural taxane via inversion of the 7-hydroxyl group simply using Ag20 as catalyst and DMF as solvent. The catalyst could he quantitatively recovered by filtra- tion without loss of catalytic activity. This condition is also applicable to the direct epimerization of taxane derivatives （e.g., docetaxel and paclitaxel） to 7-epi-taxane derivatives （e.g., 7-epi-docetaxel and 7-epi-paclitaxel）. Furthermore, 33 ester derivatives of 7-epi-taxane with different amino acid moieties at the position of C-13 were successfully synthesized via esterification without protecting C-7-OH. Bioassay results revealed that compounds 13 and 18 have good selectivity against prostatic cancer cell line DU145, with ICs0 value as low as 15.9 nmol/L for 18.

关键词： taxane 7-epi-taxane silver oxide amino acid C-13 derivative of taxane anticancer activity

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