(Q34270677)

1 August 2017

title

An update on dual Src/Abl inhibitors (English)

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1 August 2017

4

Maurizio Botta

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1 August 2017

Francesca Musumeci

1

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1 August 2017

Silvia Schenone

series ordinal

2

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1 August 2017

Chiara Brullo

series ordinal

3

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1 August 2017

publication date

1 April 2012

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Future Medicinal Chemistry

1 August 2017

published in

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1 August 2017

volume

4

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1 August 2017

issue

6

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1 August 2017

page(s)

799-822

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Structural basis for the autoinhibition of c-Abl tyrosine kinase

1 August 2017

cites work

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Last findings on dual inhibitors of abl and SRC tyrosine-kinases.

21 January 2018

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Role of Src expression and activation in human cancer

21 January 2018

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Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia

21 January 2018

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The Src family kinase Hck couples BCR/ABL to STAT5 activation in myeloid leukemia cells.

21 January 2018

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Effects of dasatinib on SRC kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells

21 January 2018

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New insights into small-molecule inhibitors of Bcr-Abl

21 January 2018

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Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia

21 January 2018

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Fatty acylation of proteins: new insights into membrane targeting of myristoylated and palmitoylated proteins

21 January 2018

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Binding of a high affinity phosphotyrosyl peptide to the Src SH2 domain: crystal structures of the complexed and peptide-free forms

21 January 2018

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Crystal structure of a Src-homology 3 (SH3) domain

21 January 2018

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Solution structure of the SH3 domain of Src and identification of its ligand-binding site

21 January 2018

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Structure and regulation of Src family kinases

21 January 2018

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A conserved salt bridge in the G loop of multiple protein kinases is important for catalysis and for in vivo Lyn function.

21 January 2018

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Crystal structures of c-Src reveal features of its autoinhibitory mechanism

21 January 2018

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The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation

21 January 2018

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A phosphotyrosine displacement mechanism for activation of Src by PTPalpha

21 January 2018

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Regulation of the c-Abl and Bcr-Abl tyrosine kinases

21 January 2018

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21 January 2018

Autoinhibition of c-Abl

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An intramolecular SH3-domain interaction regulates c-Abl activity

21 January 2018

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Phosphorylation and structure-based functional studies reveal a positive and a negative role for the activation loop of the c-Abl tyrosine kinase.

21 January 2018

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A Src-like inactive conformation in the abl tyrosine kinase domain

21 January 2018

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Mechanisms of transformation by the BCR-ABL oncogene: new perspectives in the post-imatinib era.

21 January 2018

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The coiled-coil domain and Tyr177 of bcr are required to induce a murine chronic myelogenous leukemia-like disease by bcr/abl.

21 January 2018

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The rationale engineering of BCR/ABL blockers: an answer to STI571 acquired resistance in leukemia treatment

21 January 2018

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T315I-mutated Bcr-Abl in chronic myeloid leukemia and imatinib: insights from a computational study

21 January 2018

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Rational design of inhibitors that bind to inactive kinase conformations

21 January 2018

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Through the "gatekeeper door": exploiting the active kinase conformation

21 January 2018

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New opportunities to treat the T315I-Bcr-Abl mutant in chronic myeloid leukaemia: tyrosine kinase inhibitors and molecules that act by alternative mechanisms

21 January 2018

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Allosteric inhibition of BCR-ABL.

21 January 2018

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Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation

21 January 2018

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The Src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases

21 January 2018

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Src family kinase inhibitor PP2 efficiently inhibits cervical cancer cell proliferation through down-regulating phospho-Src-Y416 and phospho-EGFR-Y1173.

21 January 2018

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Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

21 January 2018

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Overriding imatinib resistance with a novel ABL kinase inhibitor

21 January 2018

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In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants

21 January 2018

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The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib

21 January 2018

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The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

21 January 2018

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Intermittent target inhibition with dasatinib 100 mg once daily preserves efficacy and improves tolerability in imatinib-resistant and -intolerant chronic-phase chronic myeloid leukemia

21 January 2018

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Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia

21 January 2018

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Results of dasatinib therapy in patients with early chronic-phase chronic myeloid leukemia

21 January 2018

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Dasatinib in the treatment of chronic myeloid leukemia in accelerated phase after imatinib failure: the START a trial

21 January 2018

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Dasatinib treatment for imatinib resistant or intolerant patients with chronic myeloid leukaemia.

21 January 2018

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Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study

21 January 2018

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Pediatric phase I trial and pharmacokinetic study of dasatinib: a report from the children's oncology group phase I consortium

21 January 2018

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Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia

21 January 2018

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Dasatinib synergizes with doxorubicin to block growth, migration, and invasion of breast cancer cells

21 January 2018

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Once-daily dasatinib: expansion of phase II study evaluating safety and efficacy of dasatinib in patients with metastatic castration-resistant prostate cancer

21 January 2018

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Phase II Study of Dasatinib in Patients With Advanced Non–Small-Cell Lung Cancer

21 January 2018

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A phase II study of dasatinib in patients with chemosensitive relapsed small cell lung cancer (Cancer and Leukemia Group B 30602).

21 January 2018

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Phase I/II study of the Src inhibitor dasatinib in combination with erlotinib in advanced non-small-cell lung cancer

21 January 2018

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Curcumin enhances dasatinib-induced inhibition of growth and transformation of colon cancer cells

21 January 2018

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Dasatinib inhibits the development of metastases in a mouse model of pancreatic ductal adenocarcinoma

21 January 2018

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Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity

21 January 2018

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3D-QSAR studies on c-Src kinase inhibitors and docking analyses of a potent dual kinase inhibitor of c-Src and c-Abl kinases

21 January 2018

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In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells

21 January 2018

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Phase II study of single-agent bosutinib, a Src/Abl tyrosine kinase inhibitor, in patients with locally advanced or metastatic breast cancer pretreated with chemotherapy

21 January 2018

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Control of mammary tumor differentiation by SKI-606 (bosutinib)

21 January 2018

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SKI-606 (Bosutinib) blocks prostate cancer invasion, growth, and metastasis in vitro and in vivo through regulation of genes involved in cancer growth and skeletal metastasis.

21 January 2018

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Src inhibitors in lung cancer: current status and future directions

21 January 2018

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Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors

21 January 2018

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Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530

21 January 2018

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N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor

21 January 2018

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The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines

21 January 2018

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Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells

21 January 2018

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Combined Src and ER blockade impairs human breast cancer proliferation in vitro and in vivo

21 January 2018

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Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530.

21 January 2018

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Src as a therapeutic target in men with prostate cancer and bone metastases

21 January 2018

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The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells.

21 January 2018

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Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: a randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial.

21 January 2018

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The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts

21 January 2018

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Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer.

21 January 2018

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Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer.

21 January 2018

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Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors

21 January 2018

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Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

21 January 2018

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Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance

21 January 2018

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Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors

21 January 2018

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Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template

21 January 2018

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9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation

21 January 2018

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AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance

21 January 2018

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AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

21 January 2018

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Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase includ

21 January 2018

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Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance

21 January 2018

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Small molecules ATP-competitive inhibitors of FLT3: a chemical overview

21 January 2018

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Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies

21 January 2018

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Chronic myeloid leukemia stem cells are not dependent on Bcr-Abl kinase activity for their survival

21 January 2018

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Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity

21 January 2018

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Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant

21 January 2018

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Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

21 January 2018

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Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML.

21 January 2018

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Discovery and characterization of novel mutant FLT3 kinase inhibitors

21 January 2018

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Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

21 January 2018

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Affinity reagents that target a specific inactive form of protein kinases

21 January 2018

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Activity of FB2, a novel dual Abl/Src tyrosine kinase inhibitor, against imatinib-resistant chronic myeloid leukemia in vivo and in vitro

21 January 2018

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Activity of the potent dual Abl/Src tyrosine kinase inhibitor FB2 against Bcr–Abl positive cell lines in vitro and in vivo

21 January 2018

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A chemical genetic method for generating bivalent inhibitors of protein kinases

21 January 2018

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Labeling of fusion proteins of O6-alkylguanine-DNA alkyltransferase with small molecules in vivo and in vitro

21 January 2018

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Bivalent inhibitors of the tyrosine kinases ABL and SRC: determinants of potency and selectivity

21 January 2018

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Pyrazolo[3,4-d]pyrimidines as potent antiproliferative and proapoptotic agents toward A431 and 8701-BC cells in culture via inhibition of c-Src phosphorylation.

21 January 2018

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Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.

21 January 2018

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Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice

21 January 2018

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Novel dual Src/Abl inhibitors for hematologic and solid malignancies

21 January 2018

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3D QSAR models built on structure-based alignments of Abl tyrosine kinase inhibitors

21 January 2018

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C6-unsubstituted pyrazolo[3,4-d]pyrimidines are dual Src/Abl inhibitors effective against imatinib mesylate resistant chronic myeloid leukemia cell lines

21 January 2018

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New SRC/ABL inhibitors for chronic myeloid leukemia therapy show selectivity for T315I ABL mutant CD34(+) cells.

21 January 2018

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Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.

21 January 2018

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New pyrazolo-[3,4-d]-pyrimidine derivative Src kinase inhibitors lead to cell cycle arrest and tumor growth reduction of human medulloblastoma cells

21 January 2018

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Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.

21 January 2018

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Novel combination treatments targeting chronic myeloid leukemia stem cells

21 January 2018

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Development of an effective therapy for chronic myelogenous leukemia

21 January 2018

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21 January 2018

Identifiers

DOI

10.4155/FMC.12.29

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1 August 2017

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