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Abstract

The present invention discloses a novel class of covalent small molecules comprising 2-amino benzophenone derivatives for targeted ferroptosis induction in cancer cells. The present invention also includes strategies for target identification, hit-to-lead optimization, and combination therapies to enhance therapeutic efficacy. A synthesis and characterization of a library of unique organic structural scaffolds encompassing natural/unnatural amino acids, aromatic and heterocyclic linkers coupled with electrophilic units possessing diverse nucleophile reactivity profiles is provided. The molecules exhibit sub-micromolar to nanomolar inhibitory potency (IC₅₀) when screened against a panel of cancer cell lines including MCF7 (breast cancer), MDA-MB-231 (triple negative breast cancer), 22Rv1 (Prostate), PC3, (prostate cancer), Jurkat J6 (acute T-cell Leukaemia), RPMI 8226 (B lymphocytes), U87MG (glioblastoma), HCT-116 (colon cancer) and A375 (melanoma)) and kidney cells (HEK293). The molecules exhibit potent antiproliferative effects across various cancer cell lines, offering a promising alternative to conventional chemotherapies with reduced side effects.

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