Výsledky vyhledávání - "Sachin Mahale"

Design, synthesis and biological evaluation of new tryptamine and tetrahydro-β-carboline-based selective inhibitors of CDK4

Autor: Stephen J. Gray, James W. Wilson, Matthew R. Smith, Robert G. Britton, Marcos D. García, Daniel P. G. Emmerson, Sachin Mahale, Bhabatosh Chaudhuri, Paul R. Jenkins

Publikováno v: Bioorganic & Medicinal Chemistry. 16:7728-7739

We present the design, synthesis and biological activity of a library of substituted (biphenylcarbonyl)-tryptamine and (biphenylcarbonyl)-tetrahydro-β-carboline compounds related to the natural product fascaplysin, as novel inhibitors of CDK4/cyclin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6cef1a75cda1721501e0b99fdf79103
https://doi.org/10.1016/j.bmc.2008.07.002

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Antitumour potential of BPT: a dual inhibitor of cdk4 and tubulin polymerization

Autor: Bhabatosh Chaudhuri, Paul R. Jenkins, Prashant Joshi, Sudhakar Manda, Sachin Mahale, Sandip B. Bharate, Ram A. Vishwakarma

Publikováno v: Cell Death & Disease

The marine natural product fascaplysin (1) is a potent Cdk4 (cyclin-dependent kinase 4)-specific inhibitor, but is toxic to all cell types possibly because of its DNA-intercalating properties. Through the design and synthesis of numerous fascaplysin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9198dc252545091b66fbe6db1b4e5e3b
https://pubmed.ncbi.nlm.nih.gov/25950473

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Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity

Autor: Bhabatosh Chaudhuri, Sonali S. Bharate, Sandip B. Bharate, Prashant Joshi, Ram A. Vishwakarma, Paul R. Jenkins, Sudhakar Manda, Sachin Mahale

Publikováno v: Journal of medicinal chemistry. 57(22)

Biphenyl-4-carboxylic acid-[2-(1H-indol-3-yl)-ethyl]-methylamide 1 (CA224) is a nonplanar analogue of fascaplysin (2) that specifically inhibits Cdk4-cyclin D1 in vitro. Compound 1 blocks the growth of cancer cells at G0/G1 phase of the cell cycle. I

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73735aed860de5cde37225dd628a2a3d
https://pubmed.ncbi.nlm.nih.gov/25368960

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Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1

Autor: A. James Wilson, Bhabatosh Chaudhuri, Yu Yam Chan, Daniel P. G. Emmerson, Marcos D. García, Sachin Mahale, Emma J. Murphy, Paul R. Jenkins, Michael P. Dickens, Carine Aubry

We present the design, synthesis and biological activity of a new series of substituted 3-(2-(1H-indol-1-yl)ethyl)-1H-indoles and 1,2-di(1H-indol-1-yl)alkanes as selective inhibitors of CDK4/cyclin D1. The compounds were designed to explore the relat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3202648fcc8e68bbedcdb54ed03e86a7

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Anticancer effects of the flavonoid diosmetin on cell cycle progression and proliferation of MDA-MB 468 breast cancer cells due to CYP1 activation

Autor: Randolph R.J. Arroo, Vasilis P. Androutsopoulos, Gerry A. Potter, Sachin Mahale

Flavonoids constitute a large class of polyphenolic compounds with cancer preventative properties. We have examined the ability of the natural flavone diosmetin to inhibit proliferation of breast adenocarcinoma MDA-MB 468 and normal breast MCF-10A ce

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e98e58b11e2984bc0893ec991356c9d0
http://hdl.handle.net/2086/2788

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Synthesis, crystal structure and biological activity of beta-carboline based selective CDK4-cyclin D1 inhibitors

Autor: A. James Wilson, Marcos D. García, Bhabatosh Chaudhuri, Daniel P. G. Emmerson, Paul R. Jenkins, Sachin Mahale

Publikováno v: Organicbiomolecular chemistry. 4(24)

The design, synthesis and biological activity of a series of non-planar dihydro-beta-carboline and beta-carboline-based derivatives of the toxic anticancer agent fascaplysin is presented. We show these compounds to be selective inhibitors of CDK4 ove

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b85f4891d54329f50cbb3a0142714652
https://pubmed.ncbi.nlm.nih.gov/17268643

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Inhibition of cancer cell growth by cyclin dependent kinase 4 inhibitors synthesized based on the structure of fascaplysin

Autor: Sachin Mahale, Michael J. Sutcliffe, Bhabatosh Chaudhuri, Jean-Didier Maréchal, Paul R. Jenkins, Carine Aubry

Publikováno v: Bioorganic chemistry. 34(5)

Tryptamine derivatives, a new structural class of cyclin dependent kinase 4 inhibitors, have been identified during extensive biological screening of synthetic molecules. The molecules were synthesized based on the structure of fascaplysin, which is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54f17fe6286068b11336a741c431ef01
https://pubmed.ncbi.nlm.nih.gov/16904725

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CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation

Autor: Michael J. Sutcliffe, Sachin Mahale, Paul R. Jenkins, Bhabatosh Chaudhuri, Jean-Didier Maréchal, Carine Aubry, A. James Wilson

Publikováno v: Bioorganicmedicinal chemistry letters. 16(16)

Tryptamine derivatives, non-planar and potentially less toxic analogues of the anti-cancer agent fascaplysin, have been synthesised. They specifically inhibit Cdk4-D1 vis a vis Cdk2-A but, unlike fascaplysin, do not bind or intercalate DNA. CA224 is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbc7f6835480bc39c092183418d332bf
https://pubmed.ncbi.nlm.nih.gov/16750360

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