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Novel Analogues (novel + analogue)
Selected AbstractsNovel Analogues of Sydnone: Synthesis, Characterization and Antibacterial Evaluation.CHEMINFORM, Issue 49 2004Mohamed A. Moustafa Abstract For Abstract see ChemInform Abstract in Full Text. [source] Selective Treatment of Cancer: Synthesis, Biological Evaluation and Structural Elucidation of Novel Analogues of the Antibiotic CC-1065 and the DuocarmycinsCHEMISTRY - A EUROPEAN JOURNAL, Issue 16 2007Abstract Novel diastereomerically pure ,- D -galactosidic prodrugs (+)- 12,a,e of the cytotoxic antibiotics CC-1065 and the duocarmycins were prepared for an antibody directed enzyme prodrug therapy (ADEPT) using 4 as a substrate via a radical cyclization to give rac - 5 and rac - 6 followed by a chromatographic resolution of the enantiomers of rac - 5, glycosidation and linkage to the DNA-binding units 10,a,e. These only slightly toxic compounds can be toxified enzymatically by an antibody,,- D -galactosidase conjugate at the surface of malignant cells to give the cytotoxic drugs, which then alkylate DNA. The new prodrugs were tested in in vitro cytotoxicity assays showing excellent QIC50 values of 4800 and 4300 for (+)- 12,a and (+)- 12,b, respectively. The absolute configuration of precursor (+)- 5 was determined by comparison of the experimental CD spectrum with the theoretically predicted CD spectra and by X-ray structure analysis. [source] N -Fluoropyridinium trifluoromethanesulfonate and 1-fluoro-2,4,6-trimethoxy-1,3,5-triazinium hexafluoroantimonate: the first experimental determination of the F,N+ bond length involving sp2 nitrogenACTA CRYSTALLOGRAPHICA SECTION C, Issue 4 2003R. Eric Banks The structures of N -fluoropyridinium trifluoromethanesulfonate, C5H5FN+·CF3O3S,, (I), and 1-fluoro-2,4,6-trimethoxy-1,3,5-triazinium hexafluoroantimonate, (C6H9FN3O3)[SbF6], (II), are presented. The N,F bond lengths in (I), a well known electrophilic fluorinating agent, and its novel analogue, (II), are 1.357,(4) and 1.354,(4),Ĺ, respectively. [source] Alkylation of azoles: Synthesis of new heterocyclic-based AT1 -non-peptide angiotensin (II) receptor antagonistsJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2007Amal Al-Azmi Several novel analogues of Losartan 2 were synthesized as potential non-peptide angiotensin (II) receptor antagonists. In these non-peptide analogues, the tetrazole and the substituted imidazole rings of Losartan 2 were replaced, respectively, by a carboxylic acid function or its methyl ester and substituted triazole, imidazole or benzimidazole moieties. The biphenyl bromide precursor 3 (BPE) used to introduce the linker between the acid/ester function and the heterocyclic moiety was synthesized using Suzuki biphenyl coupling and then incorporated into the target molecule by simple nucleophilic substitution. The fixed N-aryl isomeric forms of several azole and benzimidazole tautomers were successfully separated by HPLC using 50% aqueous acetonitrile as eluent. Intermediate reaction products and final target compounds were fully characterized spectroscopically. [source] |