Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors

2009 ◽  
Vol 44 (2) ◽  
pp. 511-518 ◽  
Author(s):  
Anne Thiry ◽  
Aurélie Delayen ◽  
Laurence Goossens ◽  
Raymond Houssin ◽  
Marie Ledecq ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
New Family ◽  
Ca Ix ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of 1,5-Naphthyridines as Topoisomerase I Inhibitors. A New Family of Antiproliferative Agents

2015 ◽  
Vol 14 (23) ◽  
pp. 2722-2728 ◽  
Author(s):  
Concepcion Alonso ◽  
Maria Fuertes ◽  
Maria Gonzalez ◽  
Alicia Rodriguez-Gascon ◽  
Gloria Rubiales ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Biological Evaluation ◽  
Antiproliferative Agents ◽  
Topoisomerase I Inhibitors ◽  
New Family ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of Thienopyrrolizines, a New Family of CDK/GSK-3 Inhibitors

2004 ◽  
Vol 19 (6) ◽  
pp. 585-593 ◽  
Author(s):  
Christophe Rochais ◽  
Elodie Lescot ◽  
Vincent Lisowski ◽  
Alban Lepailleur ◽  
Jana sopkova-de oliveira Santos ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
New Family ◽  
Synthesis And Biological Evaluation

scholarly journals Novel Diamide-Based Benzenesulfonamides as Selective Carbonic Anhydrase IX Inhibitors Endowed with Antitumor Activity: Synthesis, Biological Evaluation and In Silico Insights

2019 ◽  
Vol 20 (10) ◽  
pp. 2484 ◽  
Author(s):  
Mohamed A. Abdelrahman ◽  
Wagdy M. Eldehna ◽  
Alessio Nocentini ◽  
Silvia Bua ◽  
Sara T. Al-Rashood ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Single Digit ◽  
Reference Drug ◽  
Docking Simulations ◽  
Ca Ix ◽  
Bioisosteric Replacement ◽  
Line Compound ◽  
Synthesis And Biological Evaluation

In this work, we present the synthesis and biological evaluation of novel series of diamide-based benzenesulfonamides 5a–h as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IX and XII. The target tumor-associated isoforms hCA IX and XII were undeniably the most affected ones (KIs: 8.3–123.3 and 9.8–134.5 nM, respectively). Notably, diamides 5a and 5h stood out as a single-digit nanomolar hCA IX inhibitors (KIs = 8.8 and 8.3 nM). The SAR outcomes highlighted that bioisosteric replacement of the benzylidene moiety, compounds 5a–g, with the hetero 2-furylidene moiety, compound 5h, achieved the best IX/I and IX/II selectivity herein reported with SIs of 985 and 13.8, respectively. Molecular docking simulations of the prepared diamides within CA IX active site revealed the ability of 5h to establish an additional H-bond between the heterocyclic oxygen and HE/Gln67. Moreover, benzenesulfonamides 5a, 5b and 5h were evaluated for their antitumor activity against renal cancer UO-31 cell line. Compound 5h was the most potent derivative with about 1.5-fold more enhanced activity (IC50 = 4.89 ± 0.22 μM) than the reference drug Staurosporine (IC50 = 7.25 ± 0.43 μM). Moreover, 5a and 5h were able to induce apoptosis in UO-31 cells as evidenced by the significant increase in the percent of annexinV-FITC positive apoptotic cells by 22.5- and 26.5-folds, respectively.

Lignopurines: A new family of hybrids between cyclolignans and purines. Synthesis and biological evaluation

2012 ◽  
Vol 58 ◽  
pp. 377-389 ◽  
Author(s):  
Ma Ángeles Castro ◽  
José Ma. Miguel del Corral ◽  
Pablo A. García ◽  
Ma Victoria Rojo ◽  
Ana C. Bento ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
New Family ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Coumarin-Linked 4-Anilinomethyl-1,2,3-Triazoles as Potent Inhibitors of Carbonic Anhydrases IX and XIII Involved in Tumorigenesis

Metabolites ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 225
Author(s):  
Pavitra S. Thacker ◽  
Prerna L. Tiwari ◽  
Andrea Angeli ◽  
Danaboina Srikanth ◽  
Baijayantimala Swain ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Molecular Hybridization ◽  
Carbonic Anhydrases ◽  
Ca Ix ◽  
Synthesis And Biological Evaluation

A series of coumarin-linked 4-anilinomethyl-1,2,3-triazoles (6a–t) was synthesized via a molecular hybridization approach, through carbon C-6 of the coumarin moiety. The synthesized compounds were evaluated for their inhibition of carbonic anhydrase (CA) isoforms I, II, IX and XIII. CAs IX and XIII were selectively inhibited over the off-target isoforms I and II. The best inhibitory profiles against CA IX were shown by compounds 6a, 6e and 6f (Ki < 50 nM), with compound 6e displaying the best inhibition with a Ki value of 36.3 nM. Compounds 6a, 6b, 6j, 6o and 6q exhibited the best inhibitory profiles against CA XIII (Ki < 100 nM). These compounds can be further explored for the discovery of potent and effective CA IX and CA XIII inhibitors.

Synthesis and Biological Evaluation of a New Family of Constrained Azabicyclic Homocholine Analogues

2010 ◽  
Vol 63 (5) ◽  
pp. 808 ◽  
Author(s):  
Jill I. Halliday ◽  
Mary Chebib ◽  
Malcolm D. McLeod
Keyword(s):  
Structural Diversity ◽  
Biological Evaluation ◽  
Ring Size ◽  
Cyclic Ketones ◽  
Nicotinic Acetylcholine ◽  
Biological Assays ◽  
New Family ◽  
Nitrogen Substitution ◽  
Receptor Targets ◽  
Synthesis And Biological Evaluation

A family of constrained acylated homocholine analogues have been synthesized, based on the azabicyclic ring scaffold derived from a double-Mannich annulation of cyclic ketones. The short synthetic route allows generation of structural diversity including, variation in the carbocyclic ring size, bridgehead substitution, nitrogen substitution and the ester sidechain. Biological assays on selected analogues demonstrate these compounds are nicotinic acetylcholine receptor (nAChR) antagonists. Several analogues also bind to other neuronal transporter and receptor targets.

scholarly journals Pyrazol(in)e derivatives of curcumin analogs as a new class of anti-Trypanosoma cruzi agents

2021 ◽  
Author(s):  
Dimitris Matiadis ◽  
Tatiana Saporiti ◽  
Elena Aguilera ◽  
Xavier Robert ◽  
Christophe Guillon ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Mammalian Cells ◽  
Triosephosphate Isomerase ◽  
Biological Evaluation ◽  
Significant Activity ◽  
New Class ◽  
New Family ◽  
Curcumin Analogs ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Aim: We report the synthesis and biological evaluation of a small library of 15 functionalized 3-styryl-2-pyrazolines and pyrazoles, derived from curcuminoids, as trypanosomicidal agents. Methods & results: The compounds were prepared via a cyclization reaction between the corresponding curcuminoids and the appropriate hydrazines. All of the derivatives synthesized were investigated for their trypanosomicidal activities. Compounds 4a and 4e showed significant activity against epimastigotes of Trypanosoma cruzi, with IC50 values of 5.0 and 4.2 μM, respectively, accompanied by no toxicity to noncancerous mammalian cells. Compound 6b was found to effectively inhibit T. cruzi triosephosphate isomerase. Conclusion: The up to 16-fold higher potency of these derivatives compared with their curcuminoid precursors makes them a promising new family of T. cruzi inhibitors.

Synthesis and Biological Evaluation of New Salvinorin B-Sulfonate Ester Ligands to Opioid Receptors

Planta Medica ◽  
2013 ◽  
Vol 79 (05) ◽  
Author(s):  
PR Polepally ◽  
BL Roth ◽  
K White ◽  
E Vardy ◽  
JK Zjawiony
Keyword(s):  
Opioid Receptors ◽  
Biological Evaluation ◽  
Sulfonate Ester ◽  
Synthesis And Biological Evaluation
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