Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides
The emergence of multidrug resistance cell lines is one of the major obstacles in the success of cancer chemotherapeutic treatment. Therefore, it remains a big challenge the development of new and effective drugs to defeat cancer. The presence of nitrogen heterocycles in the architectural design of...
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2017
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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v27_n16_p3674_Avanzo http://hdl.handle.net/20.500.12110/paper_0960894X_v27_n16_p3674_Avanzo |
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paper:paper_0960894X_v27_n16_p3674_Avanzo2023-06-08T15:57:52Z Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides 1,2,4-Oxadiazole 1,2,4-Triazole 5-Amino-1,3,4-thiadiazole Antiproliferative activity D-Ribose (5 aryl oxadiazole 3 yl) methyl dextro ribofuranoside derivative antineoplastic agent unclassified drug antineoplastic agent oxadiazole derivative ribose A-549 cell line antineoplastic activity antiproliferative activity apoptosis Article cell proliferation colon cancer cell line controlled study drug synthesis G1 phase cell cycle checkpoint HeLa cell line human human cell in vitro study lymphoma cell line prostate cancer cell line renal cancer cell line structure activity relation analogs and derivatives chemistry drug effects drug screening synthesis tumor cell line Antineoplastic Agents Cell Line, Tumor Cell Proliferation Drug Screening Assays, Antitumor Humans Oxadiazoles Ribose Structure-Activity Relationship The emergence of multidrug resistance cell lines is one of the major obstacles in the success of cancer chemotherapeutic treatment. Therefore, it remains a big challenge the development of new and effective drugs to defeat cancer. The presence of nitrogen heterocycles in the architectural design of drugs has led to the discovery of new leading compounds. Herein, we report the synthesis, characterization and in vitro antiproliferative activity against six cancer cell lines of D-ribofuranoside derivatives bearing a 1,2,4-oxadiazolic ring, with the aim of developing new active compounds. Most of these derivatives exhibit significant antiproliferative activities in the micromolar range. Noteworthy, the most potent compound of the series showed better selectivity towards the more resistant colon cancer cell line WiDr. © 2017 Elsevier Ltd 2017 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v27_n16_p3674_Avanzo http://hdl.handle.net/20.500.12110/paper_0960894X_v27_n16_p3674_Avanzo |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
1,2,4-Oxadiazole 1,2,4-Triazole 5-Amino-1,3,4-thiadiazole Antiproliferative activity D-Ribose (5 aryl oxadiazole 3 yl) methyl dextro ribofuranoside derivative antineoplastic agent unclassified drug antineoplastic agent oxadiazole derivative ribose A-549 cell line antineoplastic activity antiproliferative activity apoptosis Article cell proliferation colon cancer cell line controlled study drug synthesis G1 phase cell cycle checkpoint HeLa cell line human human cell in vitro study lymphoma cell line prostate cancer cell line renal cancer cell line structure activity relation analogs and derivatives chemistry drug effects drug screening synthesis tumor cell line Antineoplastic Agents Cell Line, Tumor Cell Proliferation Drug Screening Assays, Antitumor Humans Oxadiazoles Ribose Structure-Activity Relationship |
| spellingShingle |
1,2,4-Oxadiazole 1,2,4-Triazole 5-Amino-1,3,4-thiadiazole Antiproliferative activity D-Ribose (5 aryl oxadiazole 3 yl) methyl dextro ribofuranoside derivative antineoplastic agent unclassified drug antineoplastic agent oxadiazole derivative ribose A-549 cell line antineoplastic activity antiproliferative activity apoptosis Article cell proliferation colon cancer cell line controlled study drug synthesis G1 phase cell cycle checkpoint HeLa cell line human human cell in vitro study lymphoma cell line prostate cancer cell line renal cancer cell line structure activity relation analogs and derivatives chemistry drug effects drug screening synthesis tumor cell line Antineoplastic Agents Cell Line, Tumor Cell Proliferation Drug Screening Assays, Antitumor Humans Oxadiazoles Ribose Structure-Activity Relationship Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| topic_facet |
1,2,4-Oxadiazole 1,2,4-Triazole 5-Amino-1,3,4-thiadiazole Antiproliferative activity D-Ribose (5 aryl oxadiazole 3 yl) methyl dextro ribofuranoside derivative antineoplastic agent unclassified drug antineoplastic agent oxadiazole derivative ribose A-549 cell line antineoplastic activity antiproliferative activity apoptosis Article cell proliferation colon cancer cell line controlled study drug synthesis G1 phase cell cycle checkpoint HeLa cell line human human cell in vitro study lymphoma cell line prostate cancer cell line renal cancer cell line structure activity relation analogs and derivatives chemistry drug effects drug screening synthesis tumor cell line Antineoplastic Agents Cell Line, Tumor Cell Proliferation Drug Screening Assays, Antitumor Humans Oxadiazoles Ribose Structure-Activity Relationship |
| description |
The emergence of multidrug resistance cell lines is one of the major obstacles in the success of cancer chemotherapeutic treatment. Therefore, it remains a big challenge the development of new and effective drugs to defeat cancer. The presence of nitrogen heterocycles in the architectural design of drugs has led to the discovery of new leading compounds. Herein, we report the synthesis, characterization and in vitro antiproliferative activity against six cancer cell lines of D-ribofuranoside derivatives bearing a 1,2,4-oxadiazolic ring, with the aim of developing new active compounds. Most of these derivatives exhibit significant antiproliferative activities in the micromolar range. Noteworthy, the most potent compound of the series showed better selectivity towards the more resistant colon cancer cell line WiDr. © 2017 Elsevier Ltd |
| title |
Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| title_short |
Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| title_full |
Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| title_fullStr |
Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| title_full_unstemmed |
Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl D-ribofuranosides |
| title_sort |
synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl d-ribofuranosides |
| publishDate |
2017 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v27_n16_p3674_Avanzo http://hdl.handle.net/20.500.12110/paper_0960894X_v27_n16_p3674_Avanzo |
| _version_ |
1768546218076536832 |