3 results about "Anti proliferative" patented technology

This invention discloses a KRAS protein degrader modified with norbornene as a hydrophobic group, its preparation method, and its applications. This invention provides a protein degrader with norbornene as the hydrophobic group and MRTX1133 as the KRAS ligand terminus, capable of selectively binding to KRAS (preferably the G12D mutant) and inducing its degradation within cells through a hydrophobic tag, thereby inhibiting downstream oncogenic signaling pathways and suppressing tumor cell proliferation. One objective of this invention is to provide a general synthetic route for this type of degrader and several preferred compound examples (denoted as P1~P7), and to demonstrate methods for detecting its KRAS degradation ability and antiproliferative activity in cell biology experiments (WB, cell viability assays, etc.).

The application discloses a STAT3 / HDAC dual-target inhibitor, a composition and application thereof. A variety of biological experiments prove that the compound has excellent anti-proliferation activity on a variety of cancer cells, has STAT3 and HDAC dual inhibition activity, and has the functions of regulating Ser727 and Tyr705 phosphorylation, and can be used as a STAT3 / HDAC dual-target inhibitor to prepare an anti-tumor and other STAT3 related disease treatment, and has a good application prospect.

This invention discloses a CDK8 / BRD4 dual-target inhibitor, its preparation method, pharmaceutical composition, and applications, relating to the field of medicinal chemistry. The multi-target inhibitory compound designed and synthesized in this invention can effectively inhibit BET and kinase protein activity. The preferred compound has an IC50 value of [missing information]. 50 The concentration can reach nanomolar levels and has excellent anti-proliferative activity against colorectal cancer cells, achieving excellent therapeutic effects at the molecular level, with a very wide range of application prospects; at the same time, the compound preparation method provided by this invention is highly versatile and suitable for various structural types.