New Isoindole‐1,3‐dione Substituted Sulfonamides as Potent Inhibitors of Carbonic Anhydrase and Acetylcholinesterase: Design, Synthesis, and Biological Evaluation

2019 ◽  
Vol 4 (45) ◽  
pp. 13347-13355 ◽  
Author(s):  
Saliha Gündoğdu ◽  
Cüneyt Türkeş ◽  
Mustafa Arslan ◽  
Yeliz Demir ◽  
Şükrü Beydemir
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of coumarin-3-carboxamides as selective carbonic anhydrase IX and XII inhibitors

2019 ◽  
Vol 86 ◽  
pp. 386-392 ◽  
Author(s):  
Pavitra S. Thacker ◽  
Mallika Alvala ◽  
Mohammed Arifuddin ◽  
Andrea Angeli ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, and Biological Evaluation of Novel Carbohydrate-Based Sulfamates as Carbonic Anhydrase Inhibitors

2011 ◽  
Vol 54 (5) ◽  
pp. 1481-1489 ◽  
Author(s):  
Marie Lopez ◽  
Jonathan Trajkovic ◽  
Laurent F. Bornaghi ◽  
Alessio Innocenti ◽  
Daniela Vullo ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Inhibitors ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Carbonic Anhydrase Inhibitors: Design, Synthesis, and Biological Evaluation of Novel Sulfonyl Semicarbazide Derivatives

2014 ◽  
Vol 5 (7) ◽  
pp. 793-796 ◽  
Author(s):  
Jayashree Pichake ◽  
Prashant S. Kharkar ◽  
Mariangela Ceruso ◽  
Claudiu T. Supuran ◽  
Mrunmayee P. Toraskar
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Inhibitors ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Hypoxia-Activated Prodrug Derivatives of Carbonic Anhydrase Inhibitors in Benzenesulfonamide Series: Synthesis and Biological Evaluation

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2347 ◽  
Author(s):  
Emilie Anduran ◽  
Ashok Aspatwar ◽  
Nanda-Kumar Parvathaneni ◽  
Dennis Suylen ◽  
Silvia Bua ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Solid Tumours ◽  
Human Cell Lines ◽  
Carbonic Anhydrases ◽  
Cell Resistance ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Compound Series

Hypoxia, a common feature of solid tumours’ microenvironment, is associated with an aggressive phenotype and is known to cause resistance to anticancer chemo- and radiotherapies. Tumour-associated carbonic anhydrases isoform IX (hCA IX), which is upregulated under hypoxia in many malignancies participating to the microenvironment acidosis, represents a valuable target for drug strategy against advanced solid tumours. To overcome cancer cell resistance and improve the efficacy of therapeutics, the use of bio-reducible prodrugs also known as Hypoxia-activated prodrugs (HAPs), represents an interesting strategy to be applied to target hCA IX isozyme through the design of selective carbonic anhydrase IX inhibitors (CAIs). Here, we report the design, synthesis and biological evaluations including CA inhibition assays, toxicity assays on zebrafish and viability assays on human cell lines (HT29 and HCT116) of new HAP-CAIs, harboring different bio-reducible moieties in nitroaromatic series and a benzenesulfonamide warhead to target hCA IX. The CA inhibition assays of this compound series showed a slight selectivity against hCA IX versus the cytosolic off-target hCA II and hCA I isozymes. Toxicity and viability assays have highlighted that the compound bearing the 2-nitroimidazole moiety possesses the lowest toxicity (LC50 of 1400 µM) and shows interesting results on viability assays.

scholarly journals Design, Synthesis, and Biological Evaluation of 1,2,3-Triazole-linked triazino[5,6-b]indole-benzene sulfonamide Conjugates as Potent Carbonic Anhydrase I, II, IX, and XIII Inhibitors

Metabolites ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 200
Author(s):  
Krishna Kartheek Chinchilli ◽  
Andrea Angeli ◽  
Pavitra S. Thacker ◽  
Laxman Naik Korra ◽  
Rashmita Biswas ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Moderate Activity ◽  
Design Synthesis ◽  
Carbonic Anhydrase I ◽  
Potent Inhibition ◽  
Lead Candidate ◽  
Synthesis And Biological Evaluation ◽  
Nanomolar Range

A series of 1,2,3-triazole-linked triazino[5,6-b]indole-benzene sulfonamide hybrids (6a–6o) was synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against the human (h) isoforms hCA I, II, XIII (cytosolic isoforms), and hCA IX (transmembrane tumor-associated isoform). The results revealed that the compounds 6a–6o exhibited Ki values in the low to medium nanomolar range against hCA II and hCA IX (Kis ranging from 7.7 nM to 41.3 nM) and higher Ki values against hCA I and hCA XIII. Compound 6i showed potent inhibition of hCA II (Ki = 7.7nM), being more effective compared to the standard inhibitor acetazolamide (AAZ) (Ki = 12.1 nM). Compounds 6b and 6d showed moderate activity against hCA XIII (Ki = 69.8 and 65.8 nM). Hence, compound 6i could be consider as potential lead candidate for the design of potent and selective hCA II inhibitors.

scholarly journals Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors

2019 ◽  
Vol 10 (8) ◽  
pp. 1205-1210 ◽  
Author(s):  
Adèle Larcher ◽  
Alessio Nocentini ◽  
Claudiu T. Supuran ◽  
Jean-Yves Winum ◽  
Arie van der Lee ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Inhibitors ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of coumarin linked 1,2,4-oxadiazoles as selective carbonic anhydrase IX and XII inhibitors

2020 ◽  
Vol 98 ◽  
pp. 103739 ◽  
Author(s):  
Pavitra S. Thacker ◽  
Andrea Angeli ◽  
Omkar S. Argulwar ◽  
Prerna L. Tiwari ◽  
Mohammed Arifuddin ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
Sign in / Sign up

Export Citation Format

Share Document