Azacyanines as Novel Topoisomerase II Alpha Inhibitors

Guloglu, Sercan
Kirmaci, Fahriye Nur
Persil Çetinkol, Özgül
Forough, Mehrdad
Gulkaya, Aybuke
Introduction: Topoisomerase II alpha (Topo II alpha) has become one of the extensively exploited targets in chemotherapy due to its role in regulating the topological constraints of DNA during replication and transcription. Small molecules targeting Topo II alpha's activity such as etoposide (VP-16) and doxorubicin are extensively used in the treatment of many different types of cancer.


New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model.
Konstantinović, J; Kiriş, Erkan; Kota, KP; Kugelman-Tonos, J; Videnović, M; Cazares, LH; Terzić, Jovanović; Verbić, TŽ; Andjelković, B; Duplantier, AJ; Bavari, S; Šolaja, BA (American Chemical Society (ACS), 2018-02-22)
The synthesis and inhibitory potencies against botulinum neurotoxin serotype A light chain (BoNT/A LC) using in vitro HPLC based enzymatic assay for various steroidal, benzothiophene, thiophene, and adamantane 4-aminoquinoline derivatives are described. In addition, the compounds were evaluated for the activity against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons. Steroidal derivative 16 showed remarkable protection (up to 89% of uncleaved SNAP-25) even when administered 30 min postin...
Adaptive neuro-fuzzy inference system (ANFIS): A new approach to predictive modeling in QSAR applications: A study of neuro-fuzzy modeling of PCP-based NMDA receptor antagonists
Buyukbingol, Erdem; Sisman, Arzu; Akyıldız, Murat; Alpaslan, Ferda Nur; Adejare, Adeboye (Elsevier BV, 2007-06-15)
This paper proposes a new method, Adaptive Neuro-Fuzzy Inference System (ANFIS) to evaluate physicochemical descriptors of certain chemical compounds for their appropriate biological activities in terms of QSAR models with the aid of artificial neural network (ANN) approach combined with the principle of fuzzy logic. The ANFIS was utilized to predict NMDA (N-methyl-D-Aspartate) receptor binding activities of phencyclidine (PCP) derivatives. A data set of 38 drug-like compounds was coded with 1244 calculated...
GOKER, H; ERTAN, R; AKGUN, H; YULUG, N (Wiley, 1991-05-01)
Synthesis and antifungal evaluation of 5-ethoxycarbonyl-2-(substituted-benzyl or phenoxymethyl)benzimidazoles are reported. Structures of the compounds were elucidated with IR-, H-1-NMR-, C-13-NMR-, mass-spectra and elemental analysis. Preliminary results show that none of the synthesized benzimidazole derivatives has antifungal activity at the concentration of 100-mu-g/ml against Candida parapsilosis, Candida stellatoidea, and Candida pseudotropicalis.
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling
Kemker, Isabell; Schnepel, Christian; Schroeder, David C.; Marıon, Antoıne; Sewald, Norbert (American Chemical Society (ACS), 2019-08-22)
Halogenated L- or D-tryptophan obtained by biocatalytic halogenation was incorporated into RGD peptides together with a variety of alkyl or aryl boronic acids. Suzuki-Miyaura cross-coupling either in solution or on-resin results in side chain-to-tail-cyclized RGD peptides, for example, with biaryl moieties, providing a new dimension of structure-activity relationships. An array of RGD peptides differing in macrocycle size, the presence of D-amino acid, N-methylation, or connectivity between the indole moiet...
Multifaceted Transport Characteristics of Nanomedicine: Needs for Characterization in Dynamic Environment
Özçelikkale, Altuğ; Han, Bumsoo (American Chemical Society (ACS), 2013-06-01)
Nanomedicine for cancer, where nanoparticles (NPs) are used to deliver drugs, imaging agents, and heat to tumors, shows great potential of improved therapeutic outcomes. In spite of promising early stage results, its clinical efficacy is still significantly limited due to complex transport barriers in vivo. These transport barriers are associated with tumor microenvironment, which is highly complex and heterogeneous and varies spatiotemporally. Thus, in order to improve the in vivo efficacy of nanomedicine,...
Citation Formats
S. Guloglu, F. N. Kirmaci, Ö. Persil Çetinkol, M. Forough, and A. Gulkaya, “Azacyanines as Novel Topoisomerase II Alpha Inhibitors,” LETTERS IN DRUG DESIGN & DISCOVERY, pp. 666–671, 2020, Accessed: 00, 2020. [Online]. Available: