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Title: 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
Authors: Alanazi, M M
Amr, M A E
Naglah, A M
Mageid, R E Abdel
Elsayed, E A
Keywords: Macrocyclic pentapeptide;Schiff bases;5α-reductase inhibitors and anti-proliferate activities
Issue Date: Jan-2020
Publisher: NISCAIR-CSIR, India
Abstract: 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.
Page(s): 60-65
ISSN: 0975-1084 (Online); 0022-4456 (Print)
Appears in Collections:JSIR Vol.79(01) [January 2020]

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