2023年12月15日 · In this study, a novel series of benzamide-based PI3K/HDAC dual inhibitors were rationally designed and synthesized. Representative compound PH14 showed potent inhibitory activity toward PI3Kα and HDAC3, with IC 50 values of …

2021年12月15日 · In this study, we developed a dual-targeting PI3K and HDAC inhibitor BEBT-908 that potently inhibits tumor cell growth and potentiates anti-PD1 therapy in mice by inducing immunogenic ferroptosis in cancer cells.

2023年12月15日 · Current PI3K/HDAC dual inhibitors commonly use hydroxamate moiety as zinc binding group, which lack HDAC isoform selectivity and have potential genotoxicity. In this study, a novel series of benzamide-based PI3K/HDAC dual …

2022年9月1日 · Our previously reported 4-methylquinazoine scaffold based PI3K/HDAC dual inhibitors could suppress the growth of solid tumors and hematologic malignancies both in vitro and in vivo, validating the potential as new therapeutic agents for cancer.

2022年11月1日 · Given the potential synergism of concurrent PI3Kδ/HDAC6 inhibition, and the drawbacks of pioneering PI3K/HDAC dual inhibitors, we discovered a novel series of dual-targeted inhibitors via building HDAC6 potency in a PI3Kδ-selective template.

2023年10月19日 · The novel bifunctional PI3K/HDAC inhibitor BEBT-908 displays synergistic anti-proliferative activity against multiple hematological malignancies in vitro and has promising anti-tumor activity in xenograft tumor models of MM with PTEN deletion, ALL with prior multidrug chemotherapy, AML with FLT3-ITD mutation, and the human lymphoma tumor cell ...

2020年3月26日 · A series of quinazolin-4-one based hydroxamic acids was rationally designed and synthesized as novel dual PI3K/HDAC inhibitors by incorporating an HDAC pharmacophore into a PI3K inhibitor (Idelalisib) via an optimized linker.

2022年1月15日 · The design strategies of PI3K/mTOR, PI3K/HDAC and PI3K/MEK dual inhibitors are discussed in this review. This review will bring inspiration to medicinal chemist to design PI3K-based dual inhibitors with better efficacy.

2021年12月15日 · In this study, we developed a dual-targeting PI3K and HDAC inhibitor BEBT-908 that potently inhibits tumor cell growth and potentiates anti-PD1 therapy in mice by inducing immunogenic ferroptosis in cancer cells.

2020年11月2日 · Histone deacetylases (HDACs) are epigenetic modifiers playing critical roles in numerous key biological functions. Inappropriate expression of HDACs and dysregulation of PI3K signaling pathway are common aberrations observed in human diseases, particularly in cancers.