Anti-proliferate Activity and 5α-reductase Inhibitors of Chiral Macrocyclic (Na-di-nicotinoyl)[L-phenylalaninyl-L-leucinyl]Pentapeptide Candidates Against LNCaP and PC-3 Prostate Cancer Cell Lines

摘要

A series of macrocyclic derivatives 2-6 were prepared using N~α-dinicotinoyl-bis[L-phenylalaninyl-L-leucyl]hydrazide 1 and cyclo pentapeptide hydrazide 2 as starting materials. The hydrazide 1 was cyclized with diaminoalkanes to macrocyclic hezaazahexaamide derivatives 3a-c, respectively. Finally, compound2 was condensed with 3,5-diacetylpyridine gave the corresponding macrocyclic Schiff base 4. Finally, condensation of 2 with substituted aromatic or heterocyclic aldehyde derivatives gave the corresponding Schiff base derivatives 5a-f and 6a-c, respectively. The synthesized compounds were screened as 5α-reductase inhibitors and anti-proliferative activity against prostate cancer cell lines.