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

[1] Synthesis and Evaluation of Antioxidant Properties of 2-Substituted Quinazolin-4(3H)-ones
Mravljak, Janez
Slavec, Lara
Hrast, Martina
Sova, Matej
MOLECULES, 2021, 26 (21):
[2] An Efficient Synthesis of 2-Substituted Quinazolin-4(3H)-ones Catalyzed by Iron(III) Chloride
Mekala, Ramamohan
Akula, Raghunadh
Kamaraju, Raghavendra Rao
Bannoth, Chandrasekhar Kothapalli
Regati, Sridhar
Sarva, Jayaprakash
SYNLETT, 2014, 25 (06) : 821 - 826
[3] Synthesis and evaluation of antiproliferative activity of novel quinazolin-4(3H)-one derivatives
Venkatesh, Ramineni
Kasaboina, Suresh
Janardhan, Sridhara
Jain, Nishant
Bantu, Rajashaker
Nagarapu, Lingaiah
MEDICINAL CHEMISTRY RESEARCH, 2016, 25 (09) : 2070 - 2081
[4] Synthesis and Cytotoxicity Screening of Piperazine-1-carbodithioate Derivatives of 2-Substituted Quinazolin-4(3H)-ones
Cao, Sheng-Li
Guo, Yan-Wen
Wang, Xian-Bo
Zhang, Mei
Feng, Yu-Ping
Jiang, Yu-Yang
Wang, Yue
Gao, Qian
Ren, Jian
ARCHIV DER PHARMAZIE, 2009, 342 (03) : 182 - 189
[5] Synthesis and biological evaluation of some new quinazolin-4(3H)-ones derivatives as anticonvulsants
Gupta, Deepak
Kumar, Rajiv
Roy, Ram Kumar
Sharma, Adish
Ali, Israr
Shamsuzzaman, Md.
MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (07) : 3282 - 3288
[6] Synthesis of Quinazolin-4(3H)-ones via a novel approach
Akbari, Ali
Zahedifar, Mahboobeh
JOURNAL OF SAUDI CHEMICAL SOCIETY, 2023, 27 (02)
[7] Synthesis and Biological Potential Assessment of 2-Substituted Quinazolin-4(3H)-ones as Inhibitors of Phosphodiesterase-I and Carbonic Anhydrase-II
Saad, Syed Muhammad
Saleem, Muhammad
Perveen, Shahnaz
Alam, Muhammad Tanveer
Khan, Khalid Mohammed
Choudhary, Muhammad Iqbal
MEDICINAL CHEMISTRY, 2015, 11 (04) : 336 - 341
[8] 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
[9] Synthesis and antiproliferative evaluation of some novel quinazolin-4(3H)-one derivatives
Salem, Marwa Sayed
Al-Mabrook, Selima Ali Mohamed
El-Hashash, Maher Abd El-Aziz Mahmoud
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2020, 57 (11) : 3898 - 3906
[10] Synthesis and evaluation of antiproliferative activity of novel quinazolin-4(3H)-one derivatives
Ramineni Venkatesh
Suresh Kasaboina
Sridhara Janardhan
Nishant Jain
Rajashaker Bantu
Lingaiah Nagarapu
Medicinal Chemistry Research, 2016, 25 : 2070 - 2081

← 1 2 3 4 5 →