Semisynthesis of some novel urea, thiourea, carbamimidothioic acid and dihydrooxazole derivatives as a new class of anticancer agents

Mostafa M. Ghorab; Mansour S. Alsaid; Saleh I. Alqasoumi; Maged S. Abdel-Kader

Semisynthesis of some novel urea, thiourea, carbamimidothioic acid and dihydrooxazole derivatives as a new class of anticancer agents

Mostafa M. Ghorab, Mansour S. Alsaid, Saleh I. Alqasoumi, Maged S. Abdel-Kader

Fharmacognosy

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

The natural alkaloid 2-amino-l-phenylpropan-1-ol (1) was utilized in the synthesis of some novel urea (3-5), thiourea (8, 9), carbamimidothioic acids (12, 13) and 4, 5-dihydrooxazoles (14, 15). The structures of the semisynthesized compounds were characterized on the basis of analytical and spectral data. The synthesized compounds were evaluated in vitro for anticancer activity against the human breast (MCF-7), human liver (HEPG2) and human colon (HCT116) cancer cell lines. Compounds 3, 5 and 8 were the most active against all the cell lines compared with doxorubicin as reference drug. Also, compound 14 exhibited higher activity against human liver (HEPG2) and human colon (HCT116) cancer cell lines when compared with doxorubicin as positive control.

Original language	English
Pages (from-to)	380-385
Number of pages	6
Journal	Latin American Journal of Pharmacy
Volume	36
Issue number	2
State	Published - 2017

Keywords

Anticancer activity
Carbamimidothioic acid
Dihydrooxazole
L-norephedrine
Thiourea
Urea

UN SDGs

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

Cite this

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title = "Semisynthesis of some novel urea, thiourea, carbamimidothioic acid and dihydrooxazole derivatives as a new class of anticancer agents",

abstract = "The natural alkaloid 2-amino-l-phenylpropan-1-ol (1) was utilized in the synthesis of some novel urea (3-5), thiourea (8, 9), carbamimidothioic acids (12, 13) and 4, 5-dihydrooxazoles (14, 15). The structures of the semisynthesized compounds were characterized on the basis of analytical and spectral data. The synthesized compounds were evaluated in vitro for anticancer activity against the human breast (MCF-7), human liver (HEPG2) and human colon (HCT116) cancer cell lines. Compounds 3, 5 and 8 were the most active against all the cell lines compared with doxorubicin as reference drug. Also, compound 14 exhibited higher activity against human liver (HEPG2) and human colon (HCT116) cancer cell lines when compared with doxorubicin as positive control.",

keywords = "Anticancer activity, Carbamimidothioic acid, Dihydrooxazole, L-norephedrine, Thiourea, Urea",

author = "Ghorab, \{Mostafa M.\} and Alsaid, \{Mansour S.\} and Alqasoumi, \{Saleh I.\} and Abdel-Kader, \{Maged S.\}",

year = "2017",

language = "English",

volume = "36",

pages = "380--385",

journal = "Latin American Journal of Pharmacy",

issn = "0326-2383",

publisher = "Colegio de Farmaceuticos de la Provincia de Buenos Aires",

number = "2",

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T1 - Semisynthesis of some novel urea, thiourea, carbamimidothioic acid and dihydrooxazole derivatives as a new class of anticancer agents

AU - Ghorab, Mostafa M.

AU - Alsaid, Mansour S.

AU - Alqasoumi, Saleh I.

AU - Abdel-Kader, Maged S.

PY - 2017

Y1 - 2017

N2 - The natural alkaloid 2-amino-l-phenylpropan-1-ol (1) was utilized in the synthesis of some novel urea (3-5), thiourea (8, 9), carbamimidothioic acids (12, 13) and 4, 5-dihydrooxazoles (14, 15). The structures of the semisynthesized compounds were characterized on the basis of analytical and spectral data. The synthesized compounds were evaluated in vitro for anticancer activity against the human breast (MCF-7), human liver (HEPG2) and human colon (HCT116) cancer cell lines. Compounds 3, 5 and 8 were the most active against all the cell lines compared with doxorubicin as reference drug. Also, compound 14 exhibited higher activity against human liver (HEPG2) and human colon (HCT116) cancer cell lines when compared with doxorubicin as positive control.

AB - The natural alkaloid 2-amino-l-phenylpropan-1-ol (1) was utilized in the synthesis of some novel urea (3-5), thiourea (8, 9), carbamimidothioic acids (12, 13) and 4, 5-dihydrooxazoles (14, 15). The structures of the semisynthesized compounds were characterized on the basis of analytical and spectral data. The synthesized compounds were evaluated in vitro for anticancer activity against the human breast (MCF-7), human liver (HEPG2) and human colon (HCT116) cancer cell lines. Compounds 3, 5 and 8 were the most active against all the cell lines compared with doxorubicin as reference drug. Also, compound 14 exhibited higher activity against human liver (HEPG2) and human colon (HCT116) cancer cell lines when compared with doxorubicin as positive control.

KW - Anticancer activity

KW - Carbamimidothioic acid

KW - Dihydrooxazole

KW - L-norephedrine

KW - Thiourea

KW - Urea

UR - http://www.scopus.com/inward/record.url?scp=85009168686&partnerID=8YFLogxK

M3 - Article

AN - SCOPUS:85009168686

SN - 0326-2383

VL - 36

SP - 380

EP - 385

JO - Latin American Journal of Pharmacy

JF - Latin American Journal of Pharmacy

IS - 2

ER -

Semisynthesis of some novel urea, thiourea, carbamimidothioic acid and dihydrooxazole derivatives as a new class of anticancer agents

Abstract

Keywords

UN SDGs

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