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Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
review article
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Europe PubMed Central
title
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
(English)
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
author
Yogesh A Sonawane
series ordinal
1
1 reference
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
Amarnath Natarajan
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6
1 reference
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Europe PubMed Central
PMC publication ID
5636177
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4 April 2020
author name string
Margaret A Taylor
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2
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
John Victor Napoleon
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3
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
Sandeep Rana
series ordinal
4
1 reference
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
Jacob I Contreras
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5
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
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4 April 2020
language of work or name
English
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publication date
3 June 2016
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
published in
Journal of Medicinal Chemistry
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
volume
59
1 reference
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Europe PubMed Central
PMC publication ID
5636177
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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
issue
19
1 reference
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
page(s)
8667-8684
1 reference
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Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
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The cyclin-dependent kinase inhibitor flavopiridol potentiates doxorubicin efficacy in advanced sarcomas: preclinical investigations and results of a phase I dose-escalation clinical trial
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The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508
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Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
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TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties
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CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells
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Synopsis of some recent tactical application of bioisosteres in drug design
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11 July 2018
Roscovitine blocks leukocyte extravasation by inhibition of cyclin-dependent kinases 5 and 9.
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11 July 2018
Cyclin-dependent kinase inhibitor, P276-00 induces apoptosis in multiple myeloma cells by inhibition of Cdk9-T1 and RNA polymerase II-dependent transcription
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11 July 2018
Novel, selective CDK9 inhibitors for the treatment of HIV infection
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11 July 2018
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration
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11 July 2018
Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents
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11 July 2018
Cyclin-dependent kinase 9-cyclin K functions in the replication stress response
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11 July 2018
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11 July 2018
55K isoform of CDK9 associates with Ku70 and is involved in DNA repair
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11 July 2018
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11 July 2018
TFIIH-associated Cdk7 kinase functions in phosphorylation of C-terminal domain Ser7 residues, promoter-proximal pausing, and termination by RNA polymerase II
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11 July 2018
Identification of flavopiridol analogues that selectively inhibit positive transcription elongation factor (P-TEFb) and block HIV-1 replication
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11 July 2018
Cell cycle kinases as therapeutic targets for cancer
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11 July 2018
Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer
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11 July 2018
TFIIH kinase places bivalent marks on the carboxy-terminal domain of RNA polymerase II.
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11 July 2018
The role of lamotrigine in the management of bipolar disorder
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11 July 2018
Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines
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11 July 2018
SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples
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11 July 2018
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing
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11 July 2018
Phosphatase PPM1A regulates phosphorylation of Thr-186 in the Cdk9 T-loop
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11 July 2018
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design
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11 July 2018
The exploration of macrocycles for drug discovery--an underexploited structural class
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11 July 2018
CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases
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11 July 2018
The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation
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11 July 2018
Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology.
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11 July 2018
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11 July 2018
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11 July 2018
Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases
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11 July 2018
Inhibition of HIV-1 replication by P-TEFb inhibitors DRB, seliciclib and flavopiridol correlates with release of free P-TEFb from the large, inactive form of the complex
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11 July 2018
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors
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11 July 2018
In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00.
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11 July 2018
Mcl-1 down-regulation potentiates ABT-737 lethality by cooperatively inducing Bak activation and Bax translocation
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11 July 2018
'Seed' analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737.
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11 July 2018
Crystal structure of human cyclin K, a positive regulator of cyclin-dependent kinase 9
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11 July 2018
The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized.
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11 July 2018
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects
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11 July 2018
AZ703, an imidazo[1,2-a]pyridine inhibitor of cyclin-dependent kinases 1 and 2, induces E2F-1-dependent apoptosis enhanced by depletion of cyclin-dependent kinase 9.
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11 July 2018
Analysis of the large inactive P-TEFb complex indicates that it contains one 7SK molecule, a dimer of HEXIM1 or HEXIM2, and two P-TEFb molecules containing Cdk9 phosphorylated at threonine 186
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11 July 2018
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization
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11 July 2018
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.
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11 July 2018
Characterization of Cdk9(55) and differential regulation of two Cdk9 isoforms
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11 July 2018
Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts.
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11 July 2018
Preclinical and clinical development of the cyclin-dependent kinase inhibitor flavopiridol
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11 July 2018
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding
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11 July 2018
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity
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11 July 2018
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.
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11 July 2018
Discovery of a novel family of CDK inhibitors with the program LIDAEUS: structural basis for ligand-induced disordering of the activation loop
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11 July 2018
Cyclin T: three forms for different roles in physiological and pathological functions
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11 July 2018
Activation of MyoD-dependent transcription by cdk9/cyclin T2
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11 July 2018
7SK small nuclear RNA binds to and inhibits the activity of CDK9/cyclin T complexes
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11 July 2018
Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo
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11 July 2018
Small molecule modulators of cyclin-dependent kinases for cancer therapy
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11 July 2018
Three RNA polymerase II carboxyl-terminal domain kinases display distinct substrate preferences
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11 July 2018
Flavopiridol inhibits P-TEFb and blocks HIV-1 replication
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11 July 2018
Requirement for a kinase-specific chaperone pathway in the production of a Cdk9/cyclin T1 heterodimer responsible for P-TEFb-mediated tat stimulation of HIV-1 transcription
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11 July 2018
Down-regulation of cyclin D1 by transcriptional repression in MCF-7 human breast carcinoma cells induced by flavopiridol
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11 July 2018
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors
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11 July 2018
Flavopiridol (L86-8275): selective antitumor activity in vitro and activity in vivo for prostate carcinoma cells
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11 July 2018
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors
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11 July 2018
Human cyclin K, a novel RNA polymerase II-associated cyclin possessing both carboxy-terminal domain kinase and Cdk-activating kinase activity
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11 July 2018
Identification of multiple cyclin subunits of human P-TEFb
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11 July 2018
Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine
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11 July 2018
Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells.
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11 July 2018
Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase.
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11 July 2018
Alteration of the phosphorylation state of p34cdc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity
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11 July 2018
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23 September 2018
Cyclin-dependent kinase inhibitors move into Phase III.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Preclinical activity of P276-00, a novel small-molecule cyclin-dependent kinase inhibitor in the therapy of multiple myeloma
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Synthesis, anti-inflammatory, analgesic and kinase (CDK-1, CDK-5 and GSK-3) inhibition activity evaluation of benzimidazole/benzoxazole derivatives and some Schiff's bases
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Concise total syntheses of variolin B and deoxyvariolin B.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Reaction of bromomethylazoles and tosylmethyl isocyanide. A novel heterocyclization method for the synthesis of the core of marine alkaloids variolins and related azolopyrimidines.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Bortezomib and flavopiridol interact synergistically to induce apoptosis in chronic myeloid leukemia cells resistant to imatinib mesylate through both Bcr/Abl-dependent and -independent mechanisms
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Total syntheses of variolin B and deoxyvariolin B.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Synthesis of 2-(pyrimidin-4-yl)indoles
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Carbodiimide-mediated preparation of the tricyclic pyrido[3',2':4,5]pyrrolo[1,2-c]pyrimidine ring system and its application to the synthesis of the potent antitumoral marine alkaloid variolin B and analog.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Phase I study of the cyclin-dependent kinase inhibitor flavopiridol in combination with paclitaxel in patients with advanced solid tumors.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
A phase II trial of the cyclin-dependent kinase inhibitor flavopiridol in patients with previously untreated stage IV non-small cell lung cancer.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
RNA synthesis block by 5, 6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) triggers p53-dependent apoptosis in human colon carcinoma cells.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Elevated expression of the apoptotic regulator Mcl-1 at the time of leukemic relapse.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Inhibition of cyclin-dependent kinases by purine analogues.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5636177
retrieved
23 September 2018
Sequential flavopiridol, cytosine arabinoside, and mitoxantrone: a phase II trial in adults with poor-risk acute myelogenous leukemia
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Pattern of Expression of Cyclin T1 in Human Tissues
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Cyclin T2A Gene Maps on Human Chromosome 2q21
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Going beyond 7 + 3 regimens in the treatment of adult acute myeloid leukemia
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Simple indole alkaloids and those with a nonrearranged monoterpenoid unit
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Indole alkaloids from the tunicate Aplidium meridianum
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Serine-7 but not serine-5 phosphorylation primes RNA polymerase II CTD for P-TEFb recognition
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Differential localization and expression of the Cdk9 42k and 55k isoforms
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9
1 reference
stated in
PubMed
reference URL
https://pubmed.ncbi.nlm.nih.gov/27171036
retrieved
12 December 2020
based on heuristic
inferred from PubMed ID database lookup
Identifiers
DOI
10.1021/ACS.JMEDCHEM.6B00150
1 reference
stated in
Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
PMC publication ID
5636177
1 reference
stated in
Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
PubMed publication ID
27171036
1 reference
stated in
Europe PubMed Central
PMC publication ID
5636177
reference URL
https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27171036%20AND%20SRC:MED&resulttype=core&format=json
retrieved
4 April 2020
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