Targeting HIF-1α by newly synthesized Indolephenoxyacetamide (IPA) analogs to induce anti-angiogenesis-mediated solid tumor suppression
| Autor: | Fares Hezam, Al-Ostoot, Ankith, Sherapura, Vigneshwaran, V, Giridhara, Basappa, Vivek, H K, Prabhakar, B T, Shaukath Ara, Khanum |
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| Rok vydání: | 2021 |
| Předmět: |
Mice
Inbred BALB C Lymphoma Neovascularization Pathologic Antineoplastic Agents Hypoxia-Inducible Factor 1 alpha Subunit Xenograft Model Antitumor Assays Rats Gene Expression Regulation Neoplastic Mice Structure-Activity Relationship Acetamides Human Umbilical Vein Endothelial Cells Animals Humans Rats Wistar Signal Transduction |
| Zdroj: | Pharmacological reports : PR. 73(5) |
| ISSN: | 2299-5684 |
| Popis: | Hypoxic microenvironment is a common feature of solid tumors, which leads to the promotion of cancer. The transcription factor, HIF-1α, expressed under hypoxic conditions stimulates tumor angiogenesis, favoring HIF-1α as a promising anticancer agent. On the other hand, synthetic Indolephenoxyacetamide derivatives are known for their pharmacological potentiality. With this background here, we have synthesized, characterized, and validated the new IPA (8a-n) analogs for anti-tumor activity.The new series of IPA (8a-n) were synthesized through a multi-step reaction sequence and characterized based on the different spectroscopic analysis FT-IR,Screening for anti-proliferative studies inferred, IPA (8k) is a lead molecule with an ICThe IPA (8k) is a potent anti-proliferative molecule with anti-angiogenic activity and specifically targets HIF1α, thereby modulates its downstream regulatory genes both in vitro and in vivo. The study provides scope for new target-specific drug development against HIF-1α for the treatment of solid tumors. |
| Databáze: | OpenAIRE |
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