Synthesis and anticancer evaluation of spermatinamine analogues

Basem Moosa; Sunil Sagar; Song Li; Luke Esau; Mandeep Kaur; Niveen M. Khashab

doi:10.1016/j.bmcl.2016.01.083

Synthesis and anticancer evaluation of spermatinamine analogues

Basem Moosa, Sunil Sagar, Song Li, Luke Esau, Mandeep Kaur, Niveen M. Khashab

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Abstract

Spermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.

Original language	English (US)
Pages (from-to)	1629-1632
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	26
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2016.01.083
State	Published - Feb 4 2016

ASJC Scopus subject areas

Biochemistry
Organic Chemistry
Drug Discovery
Pharmaceutical Science
Molecular Medicine
Molecular Biology
Clinical Biochemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2016.01.083

https://repository.kaust.edu.sa/bitstream/10754/595859/1/1-s2.0-S0960894X16300919-main.pdf

Cite this

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title = "Synthesis and anticancer evaluation of spermatinamine analogues",

abstract = "Spermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.",

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T1 - Synthesis and anticancer evaluation of spermatinamine analogues

AU - Moosa, Basem

AU - Sagar, Sunil

AU - Li, Song

AU - Esau, Luke

AU - Kaur, Mandeep

AU - Khashab, Niveen M.

N1 - KAUST Repository Item: Exported on 2020-10-01

PY - 2016/2/4

Y1 - 2016/2/4

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AB - Spermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.

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JO - Bioorganic & Medicinal Chemistry Letters

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Synthesis and anticancer evaluation of spermatinamine analogues

Abstract

ASJC Scopus subject areas

UN SDGs

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