دورية أكاديمية
أعرض في EDS

Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity.

التفاصيل البيبلوغرافية
العنوان: Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity.
المؤلفون: Angeli A; University of Florence, NEUROFARBA Dept, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy; Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, 'Petru Poni' Institute of Macromolecular Chemistry, 700487 Iasi, Romania. Electronic address: andrea.angeli@unifi.it., Pinteala M; Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, 'Petru Poni' Institute of Macromolecular Chemistry, 700487 Iasi, Romania., Maier SS; Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, 'Petru Poni' Institute of Macromolecular Chemistry, 700487 Iasi, Romania; Polymers Research Center, 'Gheorghe Asachi' Technical University of Iasi, 700487 Iasi, Romania., Toti A; NEUROFARBA Department, Section of Pharmacology and Toxicology, Università degli Studi di Firenze, Viale Pieraccini 6, 50139, Florence, Italy., Di Cesare Mannelli L; NEUROFARBA Department, Section of Pharmacology and Toxicology, Università degli Studi di Firenze, Viale Pieraccini 6, 50139, Florence, Italy., Ghelardini C; NEUROFARBA Department, Section of Pharmacology and Toxicology, Università degli Studi di Firenze, Viale Pieraccini 6, 50139, Florence, Italy., Selleri S; University of Florence, NEUROFARBA Dept, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy., Carta F; University of Florence, NEUROFARBA Dept, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy., Supuran CT; University of Florence, NEUROFARBA Dept, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy.
المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Aug 01; Vol. 45, pp. 128147. Date of Electronic Publication: 2021 May 27.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
أسماء مطبوعة: Publication: Oxford : Elsevier Science Ltd
Original Publication: Oxford ; New York : Pergamon Press, c1991-
مواضيع طبية MeSH: Antineoplastic Agents/*pharmacology , Carbonic Anhydrase Inhibitors/*pharmacology , Carbonic Anhydrases/*metabolism , Sulfonamides/*pharmacology , Tellurium/*pharmacology, Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Carbonic Anhydrase Inhibitors/chemical synthesis ; Carbonic Anhydrase Inhibitors/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Molecular Structure ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/chemistry ; Tellurium/chemistry
مستخلص: We evaluated in vitro a series of telluride containing compounds bearing the benzenesulfonamide group, as effective inhibitors of the physiologically relevant human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) enzymes I, II, IV VII and IX. The potent effects of such compounds against the tumor-associated hCA IX being low nanomolar inhibitors (K I 2.2 to 2.9 nM) and with good selectivity over the ubiquitous hCA II, gave the possibility to evaluate their lethal effect in vitro against a breast cancer cell line (MDA-MB-231). Among the series, both compounds 3a and 3g induced significant toxic effects against tumor cells after 48 h incubation. Under normoxic condition 3a showed high efficacy killing over 94% of tumor cells at 1 µM, and derivative 3g reached the tumor cell viability under the 5% at 10 µM. In hypoxic condition, these two compounds showed less effective although retained excellent cancer cell killer. These unusual features make them interesting lead compounds acting as antitumor agents also in tumor types not dependent from hCA IX overexpression.
(Copyright © 2021 Elsevier Ltd. All rights reserved.)
فهرسة مساهمة: Keywords: Antitumor; Carbonic anhydrase; Inhibitor; Metalloenzymes; Organotelluride; Tellurium
المشرفين على المادة: 0 (Antineoplastic Agents)
0 (Carbonic Anhydrase Inhibitors)
0 (Isoenzymes)
0 (Sulfonamides)
EC 4.2.1.1 (Carbonic Anhydrases)
NQA0O090ZJ (Tellurium)
تواريخ الأحداث: Date Created: 20210530 Date Completed: 20220105 Latest Revision: 20220105
رمز التحديث: 20240628
DOI: 10.1016/j.bmcl.2021.128147
PMID: 34052322
قاعدة البيانات: MEDLINE
الوصف
تدمد:1464-3405
DOI:10.1016/j.bmcl.2021.128147