Search PubMed⌕ Search

Biomedical subjects

Viktor Krchnák

Publications and source records attributed to Viktor Krchnák.

11 recordsLinked to original sources
PubMed2006

Synthesis and screening of N-alkyl hydroxamates for inhibition of cancer cell proliferation.

A small library of N-alkylated amino acid-derived sulfonamide hydroxamates was synthesized on solid phase and tested for inhibition of proliferation of the highly invasive breast cancer cell line MDA-MB-231. The most active compound 4317 inhibited cell growth at IC(50) 30 microM. N-alkylation of N-H hydroxamate-based MMP inhibitors, a modification known to eliminate MMP activity, enhanced cell proliferation inhibition potency.

Antineoplastic Agents↗
PubMed2006

Solid-phase synthesis of biologically interesting compounds containing hydroxamic acid moiety.

Chemical strategies developed for the solid-phase synthesis of hydroxamates are divided into four groups: (i) the traditional synthesis of hydroxamates via cleavage of resin-bound esters by hydroxylamine and its derivatives, (ii) introduction of hydroxamic acid moiety on the resin-bound precursor, (iii) transformation of polymer-supported hydroxylamine, attached to a solid supported linker either by oxygen (O-linking strategy) or by nitrogen (N-linking strategy), and (iv) synthesis of N-alkyl hydroxamates. The scope and limitation of individual approaches are discussed.

Arylsulfonates↗
PubMed2004

Synthesis of readily cleavable immobilized 1,10-phenanthroline resins.

1,10-Phenanthroline is derivatized and ultimately immobilized on two different polystyrene/divinylbenzene solid supports using convenient methodology. All syntheses are amenable to semiautomatic processing and are scalable for high-throughput screening. A domino copper-catalyzed coupling-cyclization reaction is used to illustrate applicability in catalytic studies.

Journal Article↗
PubMedDate not supplied

Identification of synthetic phosphatidylserine translocases from a combinatorial library prepared by directed split-and-pool synthesis.

Simple sulfonamide and amide derivatives of tris(2-aminoethyl)amine (Tren) are known to promote the translocation or flip-flop of phosphatidylcholine, but not phosphatidylserine, across bilayer membranes. This paper describes the synthesis of a 300-member, spatially encoded library of Tren derivatives with appended peptide--sulfonamide and peptide--urea arms. The library was synthesized using the Encore method with SynPhase lanterns as the solid support. A high-throughput assay was developed to screen individual members of the library for an ability to translocate a fluorescent NBD derivative of phosphatidylserine across vesicle membranes. Several lead compounds were identified, and one was synthesized independently to confirm its high phosphatidylserine translocation activity.

Combinatorial Chemistry Techniques↗