Affiliation:
1. Department of Pharmacy, NMPA Key Laboratory for Clinical Research and Evaluation of Innovative Drug, West China
Hospital, Sichuan University, Chengdu, 610041, China
2. Clinical Trial Center, West China Hospital, Sichuan University, Chengdu, 610041, China
3. Department of Biotherapy, Cancer Center and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China
Abstract
Background:
Breast cancer has always been a vicious disease that threatens female
health. Although the existing surgery, radiotherapy, chemotherapy, and kinase-targeted drugs
have achieved certain effects, there are still many shortcomings. Novel compounds used to treat
breast cancer, particularly TNBC, are eagerly being discovered.
Methods:
More than 100 novel compounds that show anti-breast cancer growth were compiled
from public databases. The compound design strategies, structure-activity relationship research,
and activity evaluation methods have also been reviewed.
Results:
These novel anti-breast cancer compounds can be divided into mechanisms of action: kinase
inhibitors, epigenetic inhibitors, dual inhibitors, degraders, metal complexes, etc. The design
strategies mainly include conformational constraint, scaffold-hopping, merging key pharmacophores,
etc. Structure-activity relationship studies of these new compounds mainly focus on increasing
activity, improving selectivity, increasing membrane permeability, reducing toxicity, improving
pharmacokinetic properties, etc.
Conclusion:
Through the structural optimization of kinase inhibitors, microtubule-targeted drugs,
and metal complexes, it is expected to obtain more advantageous breast cancer treatment drugs. It
cannot be ignored that epigenetic inhibitors, dual inhibitors and degraders may bring new breast
cancer treatment strategies.
Funder
China Postdoctoral Science Foundation
Sichuan University postdoctoral interdisciplinary Innovation Fund
Fundamental Research Funds for the Central Universities
Post-Doctor Research Project, West China Hospital, Sichuan University
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,General Medicine