靶向酪氨酸激酶：吖啶酮-吡咯-吲哚酮杂合体的开发用于治疗人类乳腺癌。
Targeting tyrosine kinase: Development of acridone - pyrrole - oxindole hybrids against human breast cancer.
机构信息
Department of Chemistry, UGC Sponsored Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India.
Department of Chemistry, UGC Sponsored Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India.
出版信息
Bioorg Med Chem Lett. 2019 Jan 1;29(1):32-35. doi: 10.1016/j.bmcl.2018.11.021. Epub 2018 Nov 10.
Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4-5.4 and 59.8 Å, respectively and they also exhibited promising ADME profile.
基于分子建模研究，对先导化合物进行了合理修饰，开发出了具有高抗肿瘤活性的化合物，对 MCF 7、MDA-MB-468 和 T-47D 人乳腺癌细胞系具有抑制作用。最有效的化合物的 Log P 和总极性表面积分别为 4.4-5.4 和 59.8 Å，并且它们还表现出有前景的 ADME 特性。
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