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

Alanazi, M M; Amr, M A E; Naglah, A M; Mageid, R E Abdel; Elsayed, E A


A series of macrocyclic derivatives 2-6 were prepared using Nα-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.


5α-reductase inhibitors; Anti-proliferate activities; Macrocyclic pentapeptide, Schiff bases

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