Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities

被引：3

作者：

Karelou, Maria ^{[1
]}

Kampasis, Dionysis ^{[1
]}

Kalampaliki, Amalia D. ^{[1
]}

Persoons, Leentje ^{[2
]}

Kraemer, Andreas ^{[3
,4
]}

Schols, Dominique ^{[2
]}

Knapp, Stefan ^{[3
,4
]}

De Jonghe, Steven ^{[2
]}

Kostakis, Ioannis K. ^{[1
]}

Nikolaropoulos, Sotiris S.

机构：

[1] Natl & Kapodistrian Univ Athens, Dept Pharm, Div Pharmaceut Chem, Athens 15771, Greece

[2] Katholieke Univ Leuven, Rega Inst Med Res, Dept Microbiol Immunol & Transplantat, Lab Virol & Chemotherapy, Herestraat 49, 3000 Leuven, B-1043 Leuven, Belgium

[3] Goethe Univ Frankfurt, Inst Pharmaceut Chem, Dept Biochem Chem & Pharm, Max von Laue Str 9, D-60438 Frankfurt, Germany

[4] Goethe Univ Frankfurt, Buchmann Inst Mol Life Sci, Struct Genom Consortium, Max von Laue Str 15, D-60438 Frankfurt, Germany

来源：

MOLECULES | 2023年 / 28卷 / 23期

关键词：

quinazolines; synthesis; anti-proliferative activity; kinase inhibition; DESIGN;

D O I：

10.3390/molecules28237912

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound 17 bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.

引用

页数：16

共 50 条

[31] Synthesis, antibacterial and antifungal activities of novel thiazolidinyl sulfonamides of quinazolin-4(3H)ones
N. B. Patel
V. N. Patel
Pharmaceutical Chemistry Journal, 2010, 44 : 438 - 445
[32] Synthesis of Quinazolin-4(3H)-ones via a novel approach
Akbari, Ali
Zahedifar, Mahboobeh
JOURNAL OF SAUDI CHEMICAL SOCIETY, 2023, 27 (02)
[33] KOtBu-BF3.OEt2 mediated synthesis of quinazolin-4(3H)-ones from 2-substituted amides with nitriles and aldehydes
Nomula, Vishnuvardhan
Rao, Sadu Nageswara
SYNTHETIC COMMUNICATIONS, 2021, 51 (17) : 2602 - 2612
[34] SYNTHESIS, ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES OF NOVEL THIAZOLIDINYL SULFONAMIDES OF QUINAZOLIN-4(3H)ONES
Patel, N. B.
Patel, V. N.
PHARMACEUTICAL CHEMISTRY JOURNAL, 2010, 44 (08) : 438 - 445
[35] Synthesis, antiviral and cytotoxic activities of SomeNovel 2,3-disubstituted quinazolin-4(3H)-ones
Selvam, Periyasamy
Rathore, Padamraj
Babu, P.
Persoons, Leentje
de Clercq, Erik
ANTIVIRAL RESEARCH, 2008, 78 (02) : A64 - A64
[36] A Simple One-Pot Synthesis of 2-Substituted Quinazolin-4(3H)-ones from 2-Nitrobenzamides by Using Sodium Dithionite
Romero, Angel H.
Salazar, Jose
Lopez, Simon E.
SYNTHESIS-STUTTGART, 2013, 45 (14): : 2043 - 2050
[37] One-pot synthesis of substituted quinazolin-4(3H)-ones under microwave irradiation
Rad-Moghadam, K
Khajavi, MS
JOURNAL OF CHEMICAL RESEARCH-S, 1998, (11): : 702 - 703
[38] A General and Facile Synthesis of Novel Polysubstituted Quinazolin-4(3H)-ones
Xin, Minhang
Gao, Ying
Xiang, Hua
Chen, Dong
He, Yi
You, Qidong
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2013, 50 (01) : 169 - 174
[39] Novel Quinolone Substituted Quinazolin-4(3H)-Ones as Anti-Inflammatory, Anticancer Agents: Synthesis and Biological Screening
Kumar, Santosh
Aghara, Jignesh Chhaganbhai
Alex, Angel Treasa
Aranjani, Jesil Mathew
Joesph, Alex
INDIAN JOURNAL OF PHARMACEUTICAL EDUCATION AND RESEARCH, 2018, 52 (04) : S268 - S276
[40] Synthesis and Biological Properties of 3-(2-Hydroxyethyl)-2-(phenylamino)quinazolin-4(3H)-ones
Yang, Xuhong
Wang, Xiang
Wu, Minghu
CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2014, 34 (05) : 1015 - 1020

← 1 2 3 4 5 →