Structure−Activity Relationships for NAMI-A-type Complexes (HL)[trans-RuCl4L(S-dmso)ruthenate(III)] (L = Imidazole, Indazole, 1,2,4-Triazole, 4-Amino-1,2,4-triazole, and 1-Methyl-1,2,4-triazole):  Aquation, Redox Properties, Protein Binding, and Antiproliferative Activity

2007 ◽  
Vol 50 (9) ◽  
pp. 2185-2193 ◽  
Author(s):  
Michael Groessl ◽  
Erwin Reisner ◽  
Christian G. Hartinger ◽  
Rene Eichinger ◽  
Olga Semenova ◽  
...  
Keyword(s):  
Protein Binding ◽  
Antiproliferative Activity ◽  
Redox Properties ◽  
Structure Activity Relationships ◽  
Structure Activity

Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells

2017 ◽  
Vol 125 ◽  
pp. 1225-1234 ◽  
Author(s):  
Virginie Bellet ◽  
Laure Lichon ◽  
Dominique P. Arama ◽  
Audrey Gallud ◽  
Vincent Lisowski ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Melanoma Cells ◽  
Structure Activity Relationships ◽  
Structure Activity

Synthesis, Antiproliferative Activity, and Structure–Activity Relationships of 3‐Aryl‐1H‐quinolin‐4‐ones

ChemMedChem ◽  
2008 ◽  
Vol 3 (7) ◽  
pp. 1077-1082 ◽  
Author(s):  
Zhu‐Ping Xiao ◽  
Huan‐Qiu Li ◽  
Lei Shi ◽  
Peng‐Cheng Lv ◽  
Zhong‐Cheng Song ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Bicyclic Basic Merbarone Analogues as Antiproliferative Agents

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 557
Author(s):  
Andrea Spallarossa ◽  
Matteo Lusardi ◽  
Chiara Caneva ◽  
Aldo Profumo ◽  
Camillo Rosano ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Side Chain ◽  
The Novel ◽  
Bioactive Conformation ◽  
Pyrimidine Derivatives ◽  
Topoisomerase Iiα ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Step Procedure ◽  
Pyrimidine Moiety

Pyrimido-pyrimidine derivatives have been developed as rigid merbarone analogues. In a previous study, these compounds showed potent antiproliferative activity and efficiently inhibited topoisomerase IIα. To further extend the structure–activity relationships on pyrimido-pyrimidines, a novel series of analogues was synthesized by a two-step procedure. Analogues 3–6 bear small alky groups at positions 1 and 3 of the pyrimido-pyrimidine scaffold whereas at position 6a (4-chloro)phenyl substituent was inserted. The basic side chains introduced at position 7 were selected on the basis of the previously developed structure–activity relationships. The antiproliferative activity of the novel compounds proved to be affected by both the nature of the basic side chain and the substituents on the pyrimido-pyrimidine moiety. Derivatives 5d and 5e were identified as the most promising molecules still showing reduced antiproliferative activity in comparison with the previously prepared pyrimido-pyrimidine analogues. In topoisomerase IIα-5d docking complex, the ligand would poorly interact with the enzyme and assume a different orientation in comparison with 1d bioactive conformation.

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