A n efficient synthesis of the chlorambucil-spermidine conjugate 4 has been achieved via NI,N*-bis-Boc-spermidine and 4 has been shown to crosslink DNA lo4 times more efficiently than chlorambucil itself.
A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.
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