نتایج جستجو برای: metalated flavopiridol
تعداد نتایج: 668 فیلتر نتایج به سال:
We report the synthesis of several unique, boron-rich pincer complexes derived from m-carborane. The SeBSe and SBS pincer ligands can be synthesized via two independent synthetic routes and are metalated with Pd(II). These structures represent unique coordinating motifs, each with a Pd-B(2) bond chelated by two thio- or selenoether ligands. This class of structures serves as the first example o...
The first metalated porphyrazinediols 11 have been prepared from (L)-(+)-dimethyl tartrate via conversion into the corresponding dispoke or 2,3-dimethoxy-2,3-butanediyl protected 2,3-dihydroxymaleonitrile, Linstead macrocyclization, transmetalation, and deprotection. Their stability is very dependent on the nature of the metal ion in the cavity of the porphyrazine. Reaction of these porphyrazin...
Robust catechol-functionalized porous organic polymers (POPs) with tunable porosities (560−1050 m/g) and degrees of functionalization were synthesized using a cobaltcatalyzed acetylene trimerization (CCAT) strategy. Post-synthesis metalation can be readily carried out with a wide range of metal precursors (Cu, Mg, and Mn salts and complexes), resulting in metalated POPs with enhanced heat of hy...
A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors.
The cyclin-dependent protein kinases are important targets in drug discovery because of their role in cell cycle regulation. In this computational study, we have applied a continuum solvent model to study the interactions between cyclin-dependent kinase 2 (CDK2) and analogues of the clinically tested anticancer agent flavopiridol. The continuum solvent model uses Coulomb's law to account for di...
The metabolism of flavopiridol (FLAP), a novel anticancer drug currently undergoing clinical development, was investigated in rat and human liver microsomes. In the presence of uridine 5'-diphosphoglucuronic acid, two biotransformation products (M1 and M2) could be detected. Formation of metabolite M1 and M2 in terms of enzymatic efficacy (Vmax/K(M)) was about 50- and 5-fold higher in rat (1.58...
Wild-type cultures of Scytalidium flavo-brunneum produce a 15-azasterol antifungal agent and a reddish brown pigment as secondary metabolites. Spontaneous mutants of S. flavo-brunneum that had simultaneously lost the ability to produce the 15-azasterol and the pigment were transformed with plasmid pSFB-1, which was obtained from wild-type S. flavo-brunneum. Each transformant possessed the plasm...
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