Anti-tumor small-molecule drug conjugate including PI3K inhibitor, and synthetic method and application of anti-tumor small-molecule drug conjugate

By coupling PI3K inhibitors with Hsp90 inhibitors to form small molecule drug conjugates, the problem of insufficient regulation of PI3K-AKT-mTOR signaling pathway by existing drugs is solved, and effective inhibition and selectivity of colorectal cancer cells is achieved.

CN119707980AActive Publication Date: 2025-03-28EAST CHINA NORMAL UNIV +1
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Patent Information

Application Number
CN202311272483.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2023-09-28
Publication Date
2025-03-28
Estimated Expiration
2043-09-28

AI Technical Summary

Technical Problem

Existing anti-tumor drugs have insufficient regulation of the PI3K-AKT-mTOR signaling pathway, resulting in activation of compensatory pathways, reducing efficacy and developing drug resistance.

Method used

A small molecule drug conjugate was developed to form cleavable or non-cleavable SMDCs by coupling a PI3K inhibitor with a Hsp90 inhibitor and using alkane chain or PEG chain of different lengths as linking chains.

Benefits of technology

This small molecule drug conjugate showed significant anti-colorectal cancer activity, excellent selectivity, can effectively inhibit the proliferation and growth of tumor cells, and reduce overall toxicity.

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Abstract

The invention innovatively provides a small molecule drug conjugate for the first time, the small molecule drug conjugate takes a PI3K inhibitor as an active drug, takes extracellular HSP90 as a targeting ligand, and takes an alkane chain, a PEG chain and a nitrogen-containing heterocyclic ring as linker, and the general formula of the small molecule drug conjugate is as shown in formula (I). The invention also discloses the small molecule drug conjugate and a preparation method thereof, and application of the small molecule drug conjugate in preparation of anti-tumor and anti-colorectal cancer drugs. The invention also provides a PI3K inhibitor and a synthesis method thereof, and application of the PI3K inhibitor in synthesis of small molecule drug conjugates and preparation of anti-tumor and anti-colorectal cancer drugs. The PI3K inhibitor has an efficient PI3K inhibition effect, an anti-tumor effect, an anti-colorectal cancer effect and the like, and has a wide potential application prospect. # imgabs0 #
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