Highly Potent Triazole-Based Tubulin Polymerization Inhibitors
نویسندگان
چکیده
منابع مشابه
Development of a triazole class of highly potent Porcn inhibitors.
The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis. We have previously discovered four molecular scaffolds harboring Porcn-inhibitory activity. Comparison of their structures led to the identification of a general scaffold that can be readily assembled by modular synthesis. We rep...
متن کاملMolecular Classification of 5-Amino-2-Aroylquinolines and 4-Aroyl-6, 7, 8-Trimethoxyquinolines as Highly Potent Tubulin Polymerization Inhibitors
Algorithms for classification and taxonomy are proposed based on criteria as information entropy and its production. It is classified a series of 5-amino-2-aroylquinolines (AAQs) and 4-aroyl-6,7,8-trimethoxyquinolines (TMQs) combretastatin analogues for anti-cancer activity. 5-Amino-6-methoxy-2-aroylquinoline AAQ showed anti-proliferative activity more potent as compared to combretastatin A-4 (...
متن کاملSynthesis of phenstatin/isocombretastatin-chalcone conjugates as potent tubulin polymerization inhibitors and mitochondrial apoptotic inducers.
A series of phenstatin/isocombretastatin–chalcones were synthesized and screened for their cytotoxic activity against various human cancer cell lines. Some representative compounds exhibited significant antiproliferative activity against a panel of sixty human cancer cell lines of the NCI, with GI50 values in the range of 0.11 to 19.0 μM. Three compounds (3b, 3c and 3e) showed a broad spectrum ...
متن کاملSynthesis and Biological Evaluation of Imidazopyrmidine-Propenone Conjugates as Potent Tubulin Polymerization Inhibitors
A library of imidazopyrimidine-propenone conjugates (8a-8g) were synthesized and evaluated for their antitumor activity against three human cancer cell lines namely prostate (DU-145), lung (A549) and breast (MCF-7) cancer. These conjugates showed good to moderate activity against the tested cell lines. Among them two conjugates (8c and 8d) showed significant antiproliferative activity against h...
متن کاملNovel indole-bearing combretastatin analogues as tubulin polymerization inhibitors
BACKGROUND The combretastatins are a class of natural stilbenoids. These molecules generally share three common structural features: a trimethoxy "A"-ring, a "B"-ring containing substituent often at C3' and C4', and an ethene bridge between the two rings, which provides necessary structural rigidity. Members of the combretastatin family possess varying ability to cause vascular disruption in tu...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2007
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm061142s