DOI: 10.1002/ardp.70322 ISSN: 0365-6233

Recent Developments and Structure–Activity Relationships of BRAF Inhibitors for Cancer Drug Discovery

Xin‐Ke Guo, Kadalipura P. Rakesh, Sahana Raju, Kothanahally S. Sharath Kumar, Hua‐Li Qin

ABSTRACT

Incorporating current structural and biochemical discoveries, this paper examines how B‐RAF inhibitors control B‐RAF, including their clinical efficacy, side effects, and important medicinal chemistry characteristics. It investigates the molecular insights that may direct the creation of more potent RAF inhibitors that can target different oncogenic B‐RAF conformations. We have discussed the advantages and disadvantages of structurally varied next‐generation RAF inhibitors that are presently undergoing preclinical and clinical trials. A few of these drug candidates have started clinical trials with promising outcomes. This review also covers the structure–activity relationship of promising bioactive B‐RAF compounds, highlights advancements in the discovery and development of B‐RAF inhibitors, and attempts to assist future drug discovery initiatives.

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