当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Mechanistic investigations on substituted benzene sulphonamides as apoptosis inducing anticancer agents.

Mechanistic investigations on substituted benzene sulphonamides as apoptosis inducing anticancer agents.

Abstract：

:In an approach to develop potent cytotoxic compounds with targeted action, a systematic methodology was employed to design and initially synthesize parent compounds A1, A8, A13 and A14 followed by synthesis of further analogs of A1 (A2-A7) and A8 (A9-A12) with characterization by IR, NMR, mass and elemental techniques. These compounds were evaluated for their in vitro anti-proliferative activities against DU-145, MCF-7, HCT-15, HT-29 cell lines and apoptosis inducing potential via various mechanistic studies. Compounds A2, A9, A10 exhibited significant cytotoxic activities compared to their parent compounds and standard drug 5-fluorouracil. Compound A2 displayed superior cytotoxicity with IC50 values less than 1 µM in most of the tested cell lines. Further, compound A2 also induced apoptosis in DU-145 cells as exemplified from DAPI staining, Annexin V-FITC assay, ROS generation and mitochondrial membrane alteration studies. The above studies depict the synthesized compound A2 as potent anticancer agent with the ability to induce apoptosis in prostate cancerous cells.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Mettu A,Talla V,Thumma S,Naikal James Prameela S

doi

10.1016/j.bioorg.2019.103539

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

103539

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)31166-6

journal_volume

95

pub_type

杂志文章

相关文献

BIOORGANIC CHEMISTRY文献大全
  • α-bisabolol β-D-fucopyranoside as a potential modulator of β-amyloid peptide induced neurotoxicity: An in vitro &in silico study.

    abstract：:Alzheimer's disease (AD) is a multifaceted neurodegenerative disorder affecting the elderly people. For the AD treatment, there is inefficiency in the existing medication, as these drugs reduce only the symptoms of the disease. Since multiple pathological proteins are involved in the development of AD, searching for a...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.102935

    authors： Jeyakumar M,Sathya S,Gandhi S,Tharra P,Suryanarayanan V,Singh SK,Baire B,Pandima Devi K

    更新日期：2019-07-01 00:00:00

  • Glycopentanolones A-D, four new geranylated quinolone alkaloids from Glycosmis pentaphylla.

    abstract：:The ethanolic extract obtained from the stems of Glycosmis pentaphylla was found to suppress antigen-mediated degranulation of rat basophilic leukemia (RBL-2H3) cells. Four new geranylated 2-quinolone alkaloids, named glycopentanolones A-D (1-4), and 12 known metabolites (5-16) were isolated from the ethanolic extract...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.03.069

    authors： Choi YH,Seo C,Jeong W,Lee JE,Lee JY,Ahn EK,Kang JS,Lee JH,Choi CW,Oh JS,Lee D,Hong SS

    更新日期：2019-06-01 00:00:00

  • Ethyl benzoate bearing pyrrolizine/indolizine moieties: Design, synthesis and biological evaluation of anti-inflammatory and cytotoxic activities.

    abstract：:Two new series of ethyl benzoate bearing pyrrolizine and indolizine moieties 8-11 were synthesized and evaluated for their anti-inflammatory and anticancer activities. Among these derivatives, compounds 9a, 10b and 11b displayed in vivo anti-inflammatory and analgesic activity comparable to ibuprofen. The acute ulcero...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103371

    authors： Attalah KM,Abdalla AN,Aslam A,Ahmed M,Abourehab MAS,ElSawy NA,Gouda AM

    更新日期：2020-01-01 00:00:00

  • The green synthesis and molecular docking of novel N-substituted rhodanines as effective inhibitors for carbonic anhydrase and acetylcholinesterase enzymes.

    abstract：:Recently, inhibition effects of enzymes such as acetylcholinesterase (AChE) and carbonic anhydrase (CA) has appeared as a promising approach for pharmacological intervention in a variety of disorders such as epilepsy, Alzheimer's disease and obesity. For this purpose, novel N-substituted rhodanine derivatives (RhAs) w...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103096

    authors： Bayindir S,Caglayan C,Karaman M,Gülcin İ

    更新日期：2019-09-01 00:00:00

  • 2,4-Diketo esters: Crucial intermediates for drug discovery.

    abstract：:Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also, many 2,4-diketo ester derivatives have bee...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2020.104343

    authors： Joksimović N,Janković N,Davidović G,Bugarčić Z

    更新日期：2020-12-01 00:00:00

  • Building fluorescent sensors for carbohydrates using template-directed polymerizations.

    abstract：:The ability to custom-make fluorescent sensors for different analytes could have a tremendous impact in a variety of areas. Template-directed polymerization or molecular imprinting seems to be a promising approach for the preparation of high-affinity and specific binding sites for different template molecules. However...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1006/bioo.2001.1219

    authors： Gao S,Wang W,Wang B

    更新日期：2001-10-01 00:00:00

  • Design, synthesis and anti-diabetic activity of triazolotriazine derivatives as dipeptidyl peptidase-4 (DPP-4) inhibitors.

    abstract：:Type 2 diabetes mellitus (T2DM) is one of the major global metabolic disorders characterized by insulin resistance and chronic hyperglycemia. Inhibition of the enzyme, dipeptidyl peptidase-4 (DPP-4) has been proved as successful and safe therapy for the treatment of T2DM since last decade. In order to design novel DPP...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.03.004

    authors： Patel BD,Bhadada SV,Ghate MD

    更新日期：2017-06-01 00:00:00

  • Expeditious and eco-friendly synthesis of new multifunctionalized pyrrole derivatives and evaluation of their antioxidant property.

    abstract：:Diminution of oxidative stress-mediated diseases is an essential pharmaceutical objective in modern biomedical research. The present work stresses upon the efficient and eco-friendly synthesis of an array of novel diversely functionalized pyrrole derivatives which are found to be antioxidants with reactive oxygen spec...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103734

    authors： Kundu T,Pramanik A

    更新日期：2020-05-01 00:00:00

  • Heterocyclic cellular lipid peroxidation inhibitors inspired by the marine antioxidant barettin.

    abstract：:The marine environment remains a rich source for the discovery and development of novel bioactive compounds. The present paper describes the design, synthesis and biological evaluation of a library of small molecule heterocyclic mimetics of the marine 2,5-diketopiperazine barettin which is a powerful natural antioxida...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.11.024

    authors： Labrière C,Andersen JH,Albrigtsen M,Hansen JH,Svenson J

    更新日期：2019-03-01 00:00:00

  • Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs.

    abstract：:Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.12.036

    authors： Jin L,Dai L,Ji M,Wang H

    更新日期：2019-04-01 00:00:00

  • Rational design of pyrrolo.

    abstract：:Models have been developed for the interaction of the pyrrolo[1,2-a]benzimidazole (PBI) antitumor agents with the two-electron activating enzyme DT-diaphorase and the DNA major groove. The DT-diaphorase model and experimental results indicate that the S-enantiomer of 3-carbamido PBI can enantioselect ovarian cancers. ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1006/bioo.2000.1183

    authors： Huang X,Suleman A,Skibo EB

    更新日期：2000-12-01 00:00:00

  • Synthesis of Mitomycin C and decarbamoylmitomycin C N6 deoxyadenosine-adducts.

    abstract：:Mitomycin C (MC), an anti-cancer drug, and its analog, decarbamoylmitomycin C (DMC), are DNA-alkylating agents. MC is currently used in the clinics and its cytotoxicity is mainly due to its ability to form Interstrand Crosslinks (ICLs) which impede DNA replication and, thereby, block cancer cells proliferation. Howeve...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103280

    authors： Zheng M,Hwang S,Snyder T,Aquilina J,Proni G,Paz MM,Pradhan P,Cheng SY,Champeil E

    更新日期：2019-11-01 00:00:00

  • Design, synthesis, molecular modeling and biological evaluation of novel 1H-pyrazolo[3,4-b]pyridine derivatives as potential anticancer agents.

    abstract：:In trying to develop new anticancer agents, a series of 1H-pyrazolo[3,4-b]pyridine derivatives was designed and synthesized. Fifteen compounds were evaluated in vitro for their anti-proliferative activity against HePG-2, MCF-7, HCT-116, and PC-3 cell lines. Additionally, DNA binding affinity of the synthesized derivat...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2016.05.006

    authors： Eissa IH,El-Naggar AM,El-Hashash MA

    更新日期：2016-08-01 00:00:00

  • Synthesis of 4,6-dideoxy-3-fluoro-2-keto-beta-D-glucopyranosyl analogues of 5-fluorouracil, N6-benzoyl adenine, uracil, thymine, N4-benzoyl cytosine and evaluation of their antitumor activities.

    abstract：:The synthesis of the unsaturated 4,6-dideoxy-3-fluoro-2-keto-beta-d-glucopyranosyl nucleosides of 5-fluorouracil (6a), N(6)-benzoyl adenine (6b), uracil (6c), thymine (6d) and N(4)-benzoyl cytosine (6e), is described. Monoiodination of compounds 1a,b, followed by acetylation, catalytic hydrogenation and finally regios...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2009.11.001

    authors： Manta S,Tsoukala E,Tzioumaki N,Kiritsis C,Balzarini J,Komiotis D

    更新日期：2010-04-01 00:00:00

  • The effective molarity (EM) puzzle in proton transfer reactions.

    abstract：:The DFT and HF calculation results for the proton transfer reactions of three different systems reveal that the reaction mechanism (transfer of a proton to a nucleophile) is largely determined by the distance between the two reactive centers (r). Systems with relatively large r values tend to abstract a proton from a ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2009.04.003

    authors： Karaman R

    更新日期：2009-08-01 00:00:00

  • Identification of 5-benzylidene-2-phenylthiazolones as potent PRMT5 inhibitors by virtual screening, structural optimization and biological evaluations.

    abstract：:Protein arginine methyltransferase 5 (PRMT5) is an epigenetics related enzyme that has been validated as an important therapeutic target for glioblastoma and mantel cell lymphoma. In the present study, 11 novel PRMT5 inhibitors with 5-benzylidene-2-phenylthiazolone scaffold were identified by molecular docking-based v...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.08.021

    authors： Zhu K,Tao H,Song JL,Jin L,Zhang Y,Liu J,Chen Z,Jiang CS,Luo C,Zhang H

    更新日期：2018-12-01 00:00:00

  • An NMR spectroscopy study of bendaline-albumin interactions.

    abstract：:The complete assignment of the 1H and 13C NMR spectra of bendaline (BNDL) was performed by mono-dimensional and homo- and hetero-correlated two-dimensional NMR experiments. The interaction between bendaline and albumin was also studied by the analysis of the motional parameters spin-lattice relaxation times, allowing ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/s0045-2068(03)00078-6

    authors： Delfini M,Bianchetti C,Di Cocco ME,Pescosolido N,Porcelli F,Rosa R,Rugo G

    更新日期：2003-10-01 00:00:00

  • Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.

    abstract：:We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2015.03.003

    authors： Kaplánek R,Jakubek M,Rak J,Kejík Z,Havlík M,Dolenský B,Frydrych I,Hajdúch M,Kolář M,Bogdanová K,Králová J,Džubák P,Král V

    更新日期：2015-06-01 00:00:00

  • An alkali tolerant α-l-rhamnosidase from Fusarium moniliforme MTCC-2088 used in de-rhamnosylation of natural glycosides.

    abstract：:Analkali tolerant α-l-rhamnosidase has been purified to homogeneity from the culture filtrate of a new fungal strain, Fusarium moniliforme MTCC-2088, using concentration by ultrafiltration and cation exchange chromatography on CM cellulose column. The molecular mass of the purified enzyme has been found to be 36.0 kDa...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.11.027

    authors： Kumar D,Yadav S,Yadava S,Yadav KDS

    更新日期：2019-03-01 00:00:00

  • Semi-synthesis of C28-modified triterpene acid derivatives from maslinic acid or corosolic acid as potential α-glucosidase inhibitors.

    abstract：:Combining two bioactive moieties by covalent bond into a novel single hybrid biological entity in view of the principle of active splicing, twenty-two C28-modified derivatives of pentacyclic dihydroxytriterpene carboxylic acids with saturated nitrogen heterocycle segments (i.e. 1-deoxynojirimycin or piperazines) have ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103694

    authors： Liu X,Zang X,Yin X,Yang W,Huang J,Huang J,Yu C,Ke C,Hong Y

    更新日期：2020-04-01 00:00:00

  • Imidazole-pyrazole hybrids: Synthesis, characterization and in-vitro bioevaluation against α-glucosidase enzyme with molecular docking studies.

    abstract：:Herein, substituted imidazole-pyrazole hybrids (2a-2n) were prepared via a multi component reaction employing pyrazole-4-carbaldehydes (1a-1d), ammonium acetate, benzil and arylamines as reactants. All the new compounds were characterized through their spectral and elemental analyses. Further these compounds were test...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.10.047

    authors： Chaudhry F,Naureen S,Ashraf M,Al-Rashida M,Jahan B,Munawar MA,Khan MA

    更新日期：2019-02-01 00:00:00

  • Suntamide A, a neuroprotective cyclic peptide from Cicadidae Periostracum.

    abstract：:Suntamide A (1), a new cyclic peptide, was isolated from Cicadidae Periostracum. The gross structure of 1 was elucidated by detailed analysis of HRMS and 1D/2D NMR spectra, and the absolute configuration was established by C3 Marfey's method. We extended our study to examine biological activity of 1, and found that 1 ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104493

    authors： Thapa P,Katila N,Choi DY,Choi H,Nam JW

    更新日期：2021-01-01 00:00:00

  • Synthesis and evaluation of novel benzotropolones as Atg4B inhibiting autophagy blockers.

    abstract：:Autophagy is an intracellular degradation/recycling pathway that provides nutrients and building blocks to cellular metabolism and keeps the cytoplasm clear of obsolete proteins and organelles. During recent years, dysregulated autophagy activity has been reported to be a characteristic of many different disease types...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.03.021

    authors： Tanc M,Cleenewerck M,Kurdi A,Roelandt R,Declercq W,De Meyer G,Augustyns K,Martinet W,Van der Veken P

    更新日期：2019-06-01 00:00:00

  • The in vitro cytotoxicity, antioxidant and antibacterial potential of Satureja hortensis L. essential oil cultivated in Egypt.

    abstract：:This study was designed to evaluate the antioxidant, antibacterial and cytotoxicity effects of Satureja hortensis (S. hortensis) essential oil (EO). The GC-MS analysis of S. hortensis EO (SEO) has identified seven compounds, representing 96.84% of the oil. The two main constituents of the oil were; carvacrol (48.51%) ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103559

    authors： Abou Baker DH,Al-Moghazy M,ElSayed AAA

    更新日期：2020-01-01 00:00:00

  • Ugi efficient synthesis, biological evaluation and molecular docking of coumarin-quinoline hybrids as apoptotic agents through mitochondria-related pathways.

    abstract：:Ugi reaction was a reliable procedure for the synthesis of new coumarin-quinoline frameworks. Excellent yields, mild reaction conditions and easily available and inexpensive starting materials are advantages of this protocol. Cytotoxic effects of fourteen products were investigated in A2780 human ovarian cancer cells....

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103147

    authors： Taheri S,Nazifi M,Mansourian M,Hosseinzadeh L,Shokoohinia Y

    更新日期：2019-10-01 00:00:00

  • Design, synthesis and molecular docking of pyrazolo [3,4d] thiazole hybrids as potential anti-HIV-1 NNRT inhibitors.

    abstract：:A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via the formation of 2-imino-...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.02.006

    authors： Kasralikar HM,Jadhavar SC,Goswami SV,Kaminwar NS,Bhusare SR

    更新日期：2019-05-01 00:00:00

  • Design, synthesis and anti leukemia cells proliferation activities of pyrimidylaminoquinoline derivatives as DOT1L inhibitors.

    abstract：:A series of novel pyrimidylaminoquinoline derivatives 8(a-i) and 9(a-i) containing amino side chain, and the bisaminoquinoline analogs 3(b-e) have been designed and synthesized by structural modifications on a lead DOT1L inhibitor, 3a. All the compounds have been evaluated for their DOT1L inhibitory activities. The re...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.07.022

    authors： Zhang L,Chen Y,Liu N,Li L,Xiao S,Li X,Chen K,Luo C,Chen S,Chen H

    更新日期：2018-10-01 00:00:00

  • Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2.

    abstract：:We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward canc...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103461

    authors： Alkahtani HM,Abdalla AN,Obaidullah AJ,Alanazi MM,Almehizia AA,Alanazi MG,Ahmed AY,Alwassil OI,Darwish HW,Abdel-Aziz AA,El-Azab AS

    更新日期：2020-01-01 00:00:00

  • Syntheses of diacyltanshinol derivatives and their suppressive effects on macrophage foam cell formation by reducing oxidized LDL uptake.

    abstract：:A series of diacyltanshinol derivatives were synthesized by esterifying the corresponding o-hydroquinones of tanshinones. The suppressive effects of the synthesized compounds on oxidized low-density lipoprotein (oxLDL) uptake and oxLDL-induced macrophage-derived foam cell formation were evaluated. Our results indicate...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2013.11.001

    authors： Cheng X,Zhang DL,Li XB,Ye JT,Shi L,Huang ZS,Gu LQ,An LK

    更新日期：2014-02-01 00:00:00

  • New bisphosphorothioates and bisphosphoroamidates: synthesis, molecular modeling and determination of insecticide and toxicological profile.

    abstract：:A series of new compounds, N,N'-bis(dialkylphosphoryl)diamines and S,S'-bis(dialkylphosphoryl)-1,3-propanedithiols were prepared by a Todd-Atherton like reaction of dialkylphosphites with symmetrical diamines and 1,3-propanedithiols in a biphasic system [F.R. Athertoon, H.T. Howard, A.R. Todd, J. Chem. Soc. (1948) 110...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2006.08.006

    authors： dos Santos VM,Sant'Anna CM,Moya Borja GE,Chaaban A,Côrtes WS,DaCosta JB

    更新日期：2007-02-01 00:00:00