Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00434
Abstract: Starting from our previously described PI3Kγ inhibitors, we describe the exploration of structure-activity relationships that led to the discovery of highly potent dual PI3Kγδ inhibitors. We explored changes in two positions of the molecules, including… read more here.
Keywords: discovery azd8154; azd8154 dual; discovery; dual pi3k ... See more keywords
Synergistic efficacy of dual PI3K-d/g inhibitor Duvelisib with Bcl2 inhibitor Venetoclax in Richter's Syndrome PDX models.
Sign Up to like & getrecommendations! Published in 2021 at "Blood"
DOI: 10.1182/blood.2020010187
Abstract: A small subset of cases of chronic lymphocytic leukemia undergoes transformation to diffuse large B-cell lymphoma, Richter's Syndrome (RS), which is associated with a poor prognosis. Conventional chemotherapy results in limited responses, underlining the need… read more here.
Keywords: pi3k; inhibitor; efficacy dual; dual pi3k ... See more keywords
The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells.
Sign Up to like & getrecommendations! Published in 2020 at "Blood advances"
DOI: 10.1182/bloodadvances.2020001800
Abstract: The in-clinic phosphatidylinositol 3-kinase (PI3K) inhibitors idelalisib (CAL-101) and duvelisib (IPI-145) have demonstrated high rates of response and progression-free survival in clinical trials of B-cell malignancies, such as chronic lymphocytic leukemia (CLL). However, a high… read more here.
Keywords: pi3k; dual pi3k; ck1 inhibitor; cll ... See more keywords
Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.875372
Abstract: The PI3K-Akt-mTOR pathway is a viable target for cancer treatment and can be used to treat various malignant tumours, including follicular lymphoma and breast cancer. Both enzymes, PI3K and mTOR, are critical in this pathway.… read more here.
Keywords: mtor inhibitors; dual pi3k; pi3k mtor; treatment ... See more keywords
Dual PI3K/Akt Inhibitors Bearing Coumarin-Thiazolidine Pharmacophores as Potential Apoptosis Inducers in MCF-7 Cells
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15040428
Abstract: Breast cancer is the most common malignancy worldwide; therefore, the development of new anticancer agents is essential for improved tumor control. By adopting the pharmacophore hybridization approach, two series of 7-hydroxyl-4-methylcoumarin hybridized with thiosemicarbazone (V–VI)… read more here.
Keywords: pi3k; pi3k akt; apoptosis; dual pi3k ... See more keywords