1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.

doi:10.1021/acs.jmedchem.6b00616

Paper

1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.

Published Jun 27, 2016 · Vito Coviello, B. Marchi, S. Sartini

Journal of medicinal chemistry

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22

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Abstract

Three novel series of 1,2-benzisothiazole derivatives have been developed as inhibitors of carbonic anhydrase isoform IX. Compounds 5c and 5j, tested in vitro on the human colon cell line HT-29, blocked the growth of cells cultured under chemically induced hypoxic conditions, displaying a specific activity against cancer cells characterized by CAIX up-regulation. Moreover, a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on cell proliferation under hypoxic conditions was demonstrated.

In Vitro Study

Study Snapshot

1,2-benzisothiazole derivatives show potential as inhibitors of carbonic anhydrase isoform IX and inhibitors of cancer cell growth under hypoxic conditions, with potential synergistic activity with SN-38 and 5-fluorouracil.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.

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References

Citations

Multiple Binding Modes of Inhibitors to Human Carbonic Anhydrases: An Update on the Design of Isoform-Specific Modulators of Activity.

This review updates the structural aspects of human carbonic anhydrase inhibitor interactions, aiding in the rational design of more selective inhibitors for biomedical applications.

Discovery of novel 1,8-naphthalimide piperazinamide based benzenesulfonamides derivatives as potent carbonic anhydrase IX inhibitors and ferroptosis inducers for the treatment of triple-negative breast cancer.

Compound 9o is a potent and selective CA IX inhibitor and ferroptosis inducer for the treatment of triple-negative breast cancer, effectively inhibiting tumor growth and metastasis in a murine breast cancer 4 T1 xenograft model.

Development of a multi-targeted chemotherapeutic approach based on G-quadruplex stabilisation and carbonic anhydrase inhibition

This study proposes a novel class of compounds that stabilize G-quadruplex structures and inhibit human carbonic anhydrases IX and XII, potentially targeting multiple cancer targets and reducing cancer cell growth.

pH regulators and their inhibitors in tumor microenvironment.

pH regulators in tumors contribute to the acidic tumor microenvironment, which can be targeted for developing small-molecule antitumor inhibitors.

Prospects for the application of inhibitors of carbonic anhydrase isoforms IX and XII in oncology

Inhibiting carbonic anhydrase isoforms IX and XII in oncology significantly increases the effectiveness of chemotherapy, suppressing tumor cell resistance and increasing tumor cell sensitivity to antitumor drugs.