Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

Menshawy A. Mohamed; Rezk R. Ayyad; Taghreed Z. Shawer; Alaa A.M. Abdel-Aziz; Adel S. El-Azab

doi:10.1016/j.ejmech.2016.02.002

Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

Menshawy A. Mohamed
, Rezk R. Ayyad
, Taghreed Z. Shawer
, Alaa A.M. Abdel-Aziz
, Adel S. El-Azab

Pharmaceutical Chemistry

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

95 Scopus citations

Abstract

A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15–21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23–29) were designed, prepared and estimated for their anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal cancer cell lines, and compound 17 showed selective effectiveness against NSC lung cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung cancer HOP-92 and renal cancer UO-31 cell lines.

Original language	English
Pages (from-to)	106-113
Number of pages	8
Journal	European Journal of Medicinal Chemistry
Volume	112
DOIs	https://doi.org/10.1016/j.ejmech.2016.02.002
State	Published - 2016

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Anticancer
Broad spectrum
NCI
Quinazoline scaffolds
Synthesis

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10.1016/j.ejmech.2016.02.002

Cite this

@article{f188270247264a359857e6426b4b45bc,

title = "Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds",

abstract = "A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15–21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23–29) were designed, prepared and estimated for their anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal cancer cell lines, and compound 17 showed selective effectiveness against NSC lung cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung cancer HOP-92 and renal cancer UO-31 cell lines.",

keywords = "Anticancer, Broad spectrum, NCI, Quinazoline scaffolds, Synthesis",

author = "Mohamed, \{Menshawy A.\} and Ayyad, \{Rezk R.\} and Shawer, \{Taghreed Z.\} and Abdel-Aziz, \{Alaa A.M.\} and El-Azab, \{Adel S.\}",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Masson SAS",

year = "2016",

doi = "10.1016/j.ejmech.2016.02.002",

language = "English",

volume = "112",

pages = "106--113",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

TY - JOUR

T1 - Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

AU - Mohamed, Menshawy A.

AU - Ayyad, Rezk R.

AU - Shawer, Taghreed Z.

AU - Abdel-Aziz, Alaa A.M.

AU - El-Azab, Adel S.

PY - 2016

Y1 - 2016

N2 - A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15–21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23–29) were designed, prepared and estimated for their anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal cancer cell lines, and compound 17 showed selective effectiveness against NSC lung cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung cancer HOP-92 and renal cancer UO-31 cell lines.

AB - A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15–21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23–29) were designed, prepared and estimated for their anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal cancer cell lines, and compound 17 showed selective effectiveness against NSC lung cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung cancer HOP-92 and renal cancer UO-31 cell lines.

KW - Anticancer

KW - Broad spectrum

KW - NCI

KW - Quinazoline scaffolds

KW - Synthesis

UR - https://www.scopus.com/pages/publications/85018193014

U2 - 10.1016/j.ejmech.2016.02.002

DO - 10.1016/j.ejmech.2016.02.002

M3 - Article

C2 - 26890117

AN - SCOPUS:85018193014

SN - 0223-5234

VL - 112

SP - 106

EP - 113

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

Abstract

UN SDGs

Keywords

Access to Document

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