bms-536924 and Neoplasms

bms-536924 has been researched along with Neoplasms* in 3 studies

Reviews

2 review(s) available for bms-536924 and Neoplasms

Article	Year
Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. Journal of medicinal chemistry, 2009, Aug-27, Volume: 52, Issue:16 Topics: Animals; Antineoplastic Agents; Drug Resistance, Neoplasm; Humans; Neoplasms; Receptor, IGF Type 1; Signal Transduction	2009
[Progress in the studies on small molecule IGF-1R inhibitors]. Yao xue xue bao = Acta pharmaceutica Sinica, 2008, Volume: 43, Issue:10 The importance of insulin-like growth factor 1 receptor (IGF-1R) signaling in malignant behaviour of tumour cells is well established. Inhibiting the activity of IGF-1R may result in striking apoptosis in malignant cells growing. IGF-1R antibodies which are currently in phase I and II clinical trials and several IGF-IR TKIs have preclinically been characterized. This review describes recent developments of small molecule tyrosine kinase inhibitors. Topics: Animals; Apoptosis; Benzimidazoles; Catechin; Cell Line, Tumor; Humans; Neoplasms; Piperazines; Protein Kinase Inhibitors; Pyridones; Pyrimidines; Pyrroles; Receptor, IGF Type 1; Signal Transduction	2008

Article

Year

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.

Journal of medicinal chemistry, 2009, Aug-27, Volume: 52, Issue:16

Topics: Animals; Antineoplastic Agents; Drug Resistance, Neoplasm; Humans; Neoplasms; Receptor, IGF Type 1; Signal Transduction

2009

[Progress in the studies on small molecule IGF-1R inhibitors].

Yao xue xue bao = Acta pharmaceutica Sinica, 2008, Volume: 43, Issue:10

The importance of insulin-like growth factor 1 receptor (IGF-1R) signaling in malignant behaviour of tumour cells is well established. Inhibiting the activity of IGF-1R may result in striking apoptosis in malignant cells growing. IGF-1R antibodies which are currently in phase I and II clinical trials and several IGF-IR TKIs have preclinically been characterized. This review describes recent developments of small molecule tyrosine kinase inhibitors.

Topics: Animals; Apoptosis; Benzimidazoles; Catechin; Cell Line, Tumor; Humans; Neoplasms; Piperazines; Protein Kinase Inhibitors; Pyridones; Pyrimidines; Pyrroles; Receptor, IGF Type 1; Signal Transduction

2008

Other Studies

1 other study(ies) available for bms-536924 and Neoplasms

Article	Year
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas Journal of medicinal chemistry, 2008, Oct-09, Volume: 51, Issue:19 We previously reported that 1 (BMS-536924), a benzimidazole inhibitor of the insulin-like growth factor-1 receptor, had demonstrated in vivo antitumor activity. This lead compound was found to have potent CYP3A4 inhibition, CYP3A4 induction mediated by PXR transactivation, poor aqueous solubility, and high plasma protein binding. Herein we disclose the evolution of this chemotype to address these issues. This effort led to 10 (BMS-695735), which exhibits improved ADME properties, a low risk for drug-drug interactions, and in vivo efficacy in multiple xenograft models. Topics: Administration, Oral; Animals; Antineoplastic Agents; Benzimidazoles; Cell Line, Tumor; Cell Proliferation; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Screening Assays, Antitumor; Humans; Mice; Mice, Nude; Molecular Structure; Neoplasm Transplantation; Neoplasms; Pregnane X Receptor; Protein Kinase Inhibitors; Pyridones; Receptor, IGF Type 1; Receptors, Steroid; Solubility; Stereoisomerism; Structure-Activity Relationship; Xenograft Model Antitumor Assays	2008

Article

Year

Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinas

Journal of medicinal chemistry, 2008, Oct-09, Volume: 51, Issue:19

We previously reported that 1 (BMS-536924), a benzimidazole inhibitor of the insulin-like growth factor-1 receptor, had demonstrated in vivo antitumor activity. This lead compound was found to have potent CYP3A4 inhibition, CYP3A4 induction mediated by PXR transactivation, poor aqueous solubility, and high plasma protein binding. Herein we disclose the evolution of this chemotype to address these issues. This effort led to 10 (BMS-695735), which exhibits improved ADME properties, a low risk for drug-drug interactions, and in vivo efficacy in multiple xenograft models.

Topics: Administration, Oral; Animals; Antineoplastic Agents; Benzimidazoles; Cell Line, Tumor; Cell Proliferation; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Screening Assays, Antitumor; Humans; Mice; Mice, Nude; Molecular Structure; Neoplasm Transplantation; Neoplasms; Pregnane X Receptor; Protein Kinase Inhibitors; Pyridones; Receptor, IGF Type 1; Receptors, Steroid; Solubility; Stereoisomerism; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2008