Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 3 de 3
Filter
Add more filters










Database
Language
Publication year range
1.
Molecules ; 28(23)2023 Dec 02.
Article in English | MEDLINE | ID: mdl-38067641

ABSTRACT

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.


Subject(s)
Antineoplastic Agents , Neoplasms , Humans , Quinazolines/pharmacology , Cell Line , Structure-Activity Relationship , Antineoplastic Agents/pharmacology
2.
Int J Mol Sci ; 24(18)2023 Sep 20.
Article in English | MEDLINE | ID: mdl-37762650

ABSTRACT

Novel amino-substituted pyridoquinazolinone derivatives have been designed and synthesized as potential c-MYC G-quadruplex (G4) ligands, employing an efficient methodology. All the new compounds exhibited moderate to good antiproliferative activity against the human osteosarcoma U2OS cell line. NMR and docking experiments revealed that the recently synthesized compounds interact with the Pu22 G-quadruplex in the c-MYC promoter region, establishing a 2:1 complex, with each molecule positioned over the tetrads at the 3'- and 5'-ends.


Subject(s)
Bone Neoplasms , G-Quadruplexes , Osteosarcoma , Humans , Cell Line , Promoter Regions, Genetic
3.
Molecules ; 25(19)2020 Oct 08.
Article in English | MEDLINE | ID: mdl-33049986

ABSTRACT

Several new amino-substituted aza-acridine derivatives bearing a basic side chain have been designed and synthesized. The antiproliferative activity of the target compounds has been evaluated against three cancer cell lines-namely HCT-116 (colorectal), the uterine sarcoma MES-SA, and its doxorubicin-resistant variant MES-SA/Dx5. A limited number of the new acridines showed marginal cytotoxicity against the tested cell lines; nevertheless, these analogues possessed a similar substitution pattern. The moderate biological activity of these derivatives was attributed to their instability in aqueous media, which has been studied by mass spectrometry and computational chemistry experiments at the density functional level of theory (DFT).


Subject(s)
Acridines/chemistry , Acridines/pharmacology , Aza Compounds/chemistry , Aza Compounds/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Doxorubicin/chemistry , Doxorubicin/pharmacology , Drug Resistance, Neoplasm/drug effects , Female , HCT116 Cells , Humans , Sarcoma/drug therapy , Uterine Neoplasms/drug therapy
SELECTION OF CITATIONS
SEARCH DETAIL
...