A QSAR Study on the 4-Substituted Coumarins as Potent Tubulin Polymerization Inhibitors
نویسندگان
چکیده
منابع مشابه
Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11β-hydroxylase.
Diseases triggered by an abnormally high level of cortisol (hypercortisolism), such as the Cushing's and metabolic syndromes, could be successfully tackled by inhibitors of CYP11B1, a steroidal cytochrome P450 enzyme that catalyzes the last hydroxylation step of the cortisol biosynthesis. Structural optimization of 7-(benzyloxy)-4-(1H-imidazol-1-ylmethyl)-2H-chromen-2-one 2, a selective aromata...
متن کاملFragment-Based Hologram QSAR Studies on a Series of 2,4-Dioxopyrimidine-1-Carboxamides As Highly Potent Inhibitors of Acid Ceramidase
A series of structurally related 2,4-dioxopyrimidine-1-carboxamide derivatives as highly potent inhibitors against acid ceramidase were subjected to hologram quantitative structure-activity relationship (HQSAR) analysis. A training set containing 24 compounds served to establish the HQSAR model. The best HQSAR model was generated using atoms, bond, connectivity, donor and acceptor as fragment d...
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 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: Advanced Pharmaceutical Bulletin
سال: 2020
ISSN: 2228-5881,2251-7308
DOI: 10.34172/apb.2020.032