Unknown

Dataset Information

0

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

ABSTRACT: A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under anchorage-independent conditions, and it also demonstrated pharmacodynamic effects and efficacy in a PTEN-deficient prostate cancer PC-3 xenograft mouse model.

SUBMITTER: Lin H 

PROVIDER: S-EPMC4025772 | biostudies-other | 2012 Jul

REPOSITORIES: biostudies-other

Json Xml
altmetric image

Publications

A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under anchorage-independent conditions, and it also demonstrated pharmacodynamic effects and efficacy in a PTEN-deficient prostate cancer PC-3 xenograft mouse model. ...[more]

Similar Datasets

Unknown Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-d]Pyrimidine Series as Novel PI3K/mTOR Inhibitors.
| S-EPMC8434050 | biostudies-literature
Unknown Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Selective PI3K? Inhibitors.
| S-EPMC6274018 | biostudies-literature
Unknown Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.
| S-EPMC7486280 | biostudies-literature
Unknown Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.
| S-EPMC4266361 | biostudies-literature
Unknown Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.
| S-EPMC4394348 | biostudies-literature
Unknown Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity.
| S-EPMC5915676 | biostudies-literature
Unknown Design, Synthesis, and Biological Evaluation of Novel Thienopyrimidine Derivatives as PI3K? Inhibitors.
| S-EPMC6804295 | biostudies-literature
Unknown Design and Synthesis of Imidazopyrazolopyridines as Novel Selective COX-2 Inhibitors.
| S-EPMC6332013 | biostudies-literature
Transcriptomics Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer
2023-11-22 | GSE228587 | GEO
Unknown Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
| S-EPMC3254106 | biostudies-literature