Structure-Based Optimization of 3-Phenyl
| Autor: | Yan, Li, Wenjie, Fan, Qineng, Gong, Jie, Tian, Mi, Zhou, Qing, Li, Laura B, Uwituze, Zhichao, Zhang, Ran, Hong, Renxiao, Wang |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Male
Dose-Response Relationship Drug Molecular Structure Cell Survival Antineoplastic Agents Apoptosis Mice SCID Neoplasms Experimental Cell Line Mice Structure-Activity Relationship Mice Inbred NOD Animals Humans Myeloid Cell Leukemia Sequence 1 Protein Drug Screening Assays Antitumor Cell Proliferation |
| Zdroj: | Journal of medicinal chemistry. 64(14) |
| ISSN: | 1520-4804 |
| Popis: | Selective Mcl-1 inhibitors may overcome the drug resistance caused by current anti-apoptotic Bcl-2 protein inhibitors in tumors with Mcl-1 overexpression. Based on previously discovered compounds with a 3-phenylthiophene-2-sulfonamide core moiety, in this work, we have obtained new compounds with improved binding affinity and/or selectivity under the guidance of structure-based design. The most potent compounds achieved sub-micromolar binding affinities to Mcl-1 ( |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|