3,5-双（3-烷基氨甲基-4-羟基亚苄基）-4-哌啶酮：一类新型强效肿瘤选择性细胞毒素。
3,5-Bis(3-alkylaminomethyl-4-hydroxybenzylidene)-4-piperidones: A Novel Class of Potent Tumor-Selective Cytotoxins.
作者信息
Karki Subhas S, Das Umashankar, Umemura Naoki, Sakagami Hiroshi, Iwamoto Shoko, Kawase Masami, Balzarini Jan, De Clercq Erik, Dimmock Stephen G, Dimmock Jonathan R
机构信息
Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan , Saskatoon, Saskatchewan S7H 5C9, Canada.
Department of Diagnostic and Therapeutic Sciences, Division of Pharmacology, Meikai University School of Dentistry , 1-1 Keyakidai, Sakado, Saitama 350-0238, Japan.
出版信息
J Med Chem. 2016 Jan 28;59(2):763-9. doi: 10.1021/acs.jmedchem.5b01706. Epub 2016 Jan 7.
Novel 4-piperidone derivatives 2a-f are disclosed as potent cytotoxins. Many of these compounds are more potent than the reference drug melphalan. The compounds in series 2, 4-7 display selective toxicities toward various neoplasms compared to some normal cells. 2a is one of the promising lead molecules that display >11-fold higher growth inhibiting potency than 5-fluorouracil against human colon cancer cells. 2a induces apoptosis, DNA fragmentation, and cleavage of poly ADP-ribose polymerase.
新型4-哌啶酮衍生物2a-f被披露为强效细胞毒素。这些化合物中的许多比参比药物美法仑更有效。与一些正常细胞相比，2、4-7系列中的化合物对各种肿瘤显示出选择性毒性。2a是有前景的先导分子之一，其对人结肠癌细胞的生长抑制效力比5-氟尿嘧啶高11倍以上。2a诱导细胞凋亡、DNA片段化以及聚ADP-核糖聚合酶的裂解。
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