can-508 and Neoplasms

can-508 has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for can-508 and Neoplasms

Article	Year
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. European journal of medicinal chemistry, 2020, Mar-01, Volume: 189 In the present study, we report the design and synthesis of novel CAN508 sulfonamide-based analogues (4, 8a-e, 9a-h and 10a-e) as novel carbonic anhydrase (CA) inhibitors with potential CDK inhibitory activity. A bioisosteric replacement approach was adopted to replace the phenolic OH of CAN508 with a sulfamoyl group to afford compound 4. Thereafter, a ring-fusion approach was utilized to furnish the 5/5 fused imidazopyrazoles 8a-e which were subsequently expanded to 6/5 pyrazolopyrimidines 9a-h and 10a-e. All the synthesized analogues were evaluated for their inhibitory activity toward isoforms hCA I, II, IX and XII. The target tumor-associated isoforms hCA IX and XII were effectively inhibited with K Topics: Antineoplastic Agents; Azo Compounds; Carbonic Anhydrase Inhibitors; Carbonic Anhydrases; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Humans; In Vitro Techniques; Molecular Docking Simulation; Molecular Structure; Neoplasms; Pyrazoles; Structure-Activity Relationship; Sulfonamides	2020

Article

Year

Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.

European journal of medicinal chemistry, 2020, Mar-01, Volume: 189

In the present study, we report the design and synthesis of novel CAN508 sulfonamide-based analogues (4, 8a-e, 9a-h and 10a-e) as novel carbonic anhydrase (CA) inhibitors with potential CDK inhibitory activity. A bioisosteric replacement approach was adopted to replace the phenolic OH of CAN508 with a sulfamoyl group to afford compound 4. Thereafter, a ring-fusion approach was utilized to furnish the 5/5 fused imidazopyrazoles 8a-e which were subsequently expanded to 6/5 pyrazolopyrimidines 9a-h and 10a-e. All the synthesized analogues were evaluated for their inhibitory activity toward isoforms hCA I, II, IX and XII. The target tumor-associated isoforms hCA IX and XII were effectively inhibited with K

Topics: Antineoplastic Agents; Azo Compounds; Carbonic Anhydrase Inhibitors; Carbonic Anhydrases; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Humans; In Vitro Techniques; Molecular Docking Simulation; Molecular Structure; Neoplasms; Pyrazoles; Structure-Activity Relationship; Sulfonamides

2020