Design, synthesis, and biological investigation of selective human carbonic anhydrase II, IX, and XII inhibitors using 7-aryl/heteroaryl triazolopyrimidines bearing a sulfanilamide scaffold

Triazole-fused pyrimidines in target-based anticancer drug discovery

(2023) Xing-Jie Dai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Carbonic Anhydrases in Metazoan Model Organisms: Molecules, Mechanisms, and Physiology

(2022) Ashok Aspatwar et al.   PHYSIOLOGICAL REVIEWS

A Decade of Tail-approach Based Design of Selective as well as Potent Tumor Associated Carbonic Anhydrase Inhibitors

(2022) Amit Kumar et al.   BIOORGANIC CHEMISTRY

Design, synthesis, biological assessment, and in-Silico studies of 1,2,4-triazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors

(2022) Heba S. Mohamed et al.   BIOORGANIC CHEMISTRY

Synthesis and Biological Evaluation of Highly Active 7-Anilino Triazolopyrimidines as Potent Antimicrotubule Agents

(2022) Paola Oliva et al.   Pharmaceutics

Benzenesulfonamides with different rigidity-conferring linkers as carbonic anhydrase inhibitors: an insight into the antiproliferative effect on glioblastoma, pancreatic, and breast cancer cells

(2022) Francesco Liguori et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Cancer Therapeutic Targeting of Hypoxia Induced Carbonic Anhydrase IX: From Bench to Bedside

(2022) Paul C. McDonald et al.   Cancers

Design, Synthesis and Biological Investigation of 2-Anilino Triazolopyrimidines as Tubulin Polymerization Inhibitors with Anticancer Activities

(2022) Romeo Romagnoli et al.   Pharmaceuticals

Microtubule-Stabilizing 1,2,4-Triazolo[1,5-a]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure–Activity Insights

(2022) Thibault Alle et al.   Journal of Medicinal Chemistry

Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities

(2021) Mostafa M. Elbadawi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Developments of small molecules as inhibitors for carbonic anhydrase isoforms

(2021) Emmanuel Ramsey Buabeng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines

(2021) Xian-Sen Huo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel carbonic anhydrase inhibitors

(2021) Claudiu T Supuran   Future Medicinal Chemistry

Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide – A new caspase-activating proapoptotic agent

(2021) Dmitry Dar'in et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Carbonic anhydrase inhibitors: an update on experimental agents for the treatment and imaging of hypoxic tumors

(2021) Claudiu T. Supuran   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action

(2020) Mohamed Fares et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Phase 1 Study of SLC-0111, a Novel Inhibitor of Carbonic Anhydrase IX, in Patients With Advanced Solid Tumors

(2020) Paul C. McDonald et al.   AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS

Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: Where are we today?

(2020) Chandra B. Mishra et al.   MEDICINAL RESEARCH REVIEWS

The Expression of Carbonic Anhydrases II, IX and XII in Brain Tumors

(2020) Joonas Haapasalo et al.   Cancers

Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis

(2020) Mohamed A. Abdelrahman et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-a]Pyrimidine Derivatives as Highly Potent and Orally Active ABCB1 Modulators

(2020) Shuai Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The role of carbonic anhydrase IX in cancer development: links to hypoxia, acidosis, and beyond

(2019) Silvia Pastorekova et al.   CANCER AND METASTASIS REVIEWS

Synthesis, structure-activity relationship studies and biological characterization of new [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1/KDM1A inhibitors

(2019) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A new widespread subclass of carbonic anhydrase in marine phytoplankton

(2019) Erik L. Jensen et al.   ISME Journal

Discovery of [1,2,4]triazolo[1,5-a]pyrimidine derivatives as new bromodomain-containing protein 4 (BRD4) inhibitors

(2019) Shuai Wang et al.   CHINESE CHEMICAL LETTERS

Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery

(2019) Alessio Nocentini et al.   Expert Opinion on Drug Discovery

Novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives as potent antitubulin agents: Design, multicomponent synthesis and antiproliferative activities

(2019) Fang Yang et al.   BIOORGANIC CHEMISTRY

Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX

(2019) Heba Abdelrasheed Allam et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors

(2019) Lalit Vats et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform

(2018) Hany S. Ibrahim et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one

(2018) Claudiu T. Supuran et al.   MEDICINAL RESEARCH REVIEWS

A surface proton antenna in carbonic anhydrase II supports lactate transport in cancer cells

(2018) Sina Ibne Noor et al.   eLife

Carbonic anhydrase IX is a pH-stat that sets an acidic tumour extracellular pH in vivo

(2018) Shen-Han Lee et al.   BRITISH JOURNAL OF CANCER

Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents

(2018) Wagdy M. Eldehna et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

SLC-0111 enaminone analogs, 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides, as novel selective subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform IX

(2018) Wagdy M. Eldehna et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors

(2017) Shuai Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Carbonic anhydrase — a universal enzyme of the carbon-based life

(2017) E. Kupriyanova et al.   PHOTOSYNTHETICA

Synthesis and Biological Evaluation of 2-Methyl-4,5-Disubstituted Oxazoles as a Novel Class of Highly Potent Antitubulin Agents

(2017) Romeo Romagnoli et al.   Scientific Reports

Structure and function of carbonic anhydrases

(2016) C. T. Supuran   BIOCHEMICAL JOURNAL

Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII

(2016) Wagdy M. Eldehna et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Advances in structure-based drug discovery of carbonic anhydrase inhibitors

(2016) Claudiu T. Supuran   Expert Opinion on Drug Discovery

Targeting carbonic anhydrase IX with small organic ligands

(2015) Moreno Wichert et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

How many carbonic anhydrase inhibition mechanisms exist?

(2015) Claudiu T. Supuran   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Carbonic Anhydrase Inhibitors with Dual-Tail Moieties To Match the Hydrophobic and Hydrophilic Halves of the Carbonic Anhydrase Active Site

(2015) Rajendra P. Tanpure et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hypoxia-induced carbonic anhydrase IX as a target for cancer therapy: From biology to clinical use

(2015) Jaromir Pastorek et al.   SEMINARS IN CANCER BIOLOGY

Carbonic anhydrase XII is a new therapeutic target to overcome chemoresistance in cancer cells

(2015) Joanna Kopecka et al.   Oncotarget

Recent Developments in Targeting Carbonic Anhydrase IX for Cancer Therapeutics

(2015) Paul C. McDonald et al.   Oncotarget

Safety of carbonic anhydrase inhibitors

(2014) Erik R Swenson   Expert Opinion On Drug Safety

Sulfonamides and their isosters as carbonic anhydrase inhibitors

(2014) Fabrizio Carta et al.   Future Medicinal Chemistry

Combining the tail and the ring approaches for obtaining potent and isoform-selective carbonic anhydrase inhibitors: Solution and X-ray crystallographic studies

(2013) Murat Bozdag et al.   BIOORGANIC & MEDICINAL CHEMISTRY

CA II, a potential biomarker by proteomic analysis, exerts significant inhibitory effect on the growth of colorectal cancer cells

(2013) RUI ZHOU et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Multiple Binding Modes of Inhibitors to Carbonic Anhydrases: How to Design Specific Drugs Targeting 15 Different Isoforms?

(2012) Vincenzo Alterio et al.   CHEMICAL REVIEWS

Structure-based drug discovery of carbonic anhydrase inhibitors

(2012) Claudiu T. Supuran   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Ureido-Substituted Benzenesulfonamides Potently Inhibit Carbonic Anhydrase IX and Show Antimetastatic Activity in a Model of Breast Cancer Metastasis

(2011) Fabio Pacchiano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Interfering with pH regulation in tumours as a therapeutic strategy

(2011) Dario Neri et al.   NATURE REVIEWS DRUG DISCOVERY

Carbonic anhydrase II. A novel biomarker for gastrointestinal stromal tumors

(2010) Seppo Parkkila et al.   MODERN PATHOLOGY

Intratumoral Hypoxic Gradient Drives Stem Cells Distribution and MGMT Expression in Glioblastoma

(2010) Francesca Pistollato et al.   STEM CELLS

Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target

(2009) Giuseppina De Simone et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Molecular Mechanisms of HIF-1α Modulation Induced by Oxygen Tension and BMP2 in Glioblastoma Derived Cells

(2009) Francesca Pistollato et al.   PLoS One

Hypoxia-Inducible Carbonic Anhydrase IX and XII Promote Tumor Cell Growth by Counteracting Acidosis through the Regulation of the Intracellular pH

(2008) J. Chiche et al.   CANCER RESEARCH

Carbonic Anhydrase as a Model for Biophysical and Physical-Organic Studies of Proteins and Protein−Ligand Binding

(2008) Vijay M. Krishnamurthy et al.   CHEMICAL REVIEWS

Cancer-Associated Carbonic Anhydrases and Their Inhibition

(2008) J. Pastorek et al.   CURRENT PHARMACEUTICAL DESIGN

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

(2008) Claudiu T. Supuran   NATURE REVIEWS DRUG DISCOVERY