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Last update 20 Mar 2025

Buciclovir

Last update 20 Mar 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious Diseases

Active Indication

Herpesviridae Infections

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseClinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC9H13N5O3

InChIKeyQOVUZUCXPAZXDZ-RXMQYKEDSA-N

CAS Registry86304-28-1

100 Clinical Results associated with Buciclovir

100 Translational Medicine associated with Buciclovir

100 Patents (Medical) associated with Buciclovir

Literatures (Medical) associated with Buciclovir

21 Dec 2018·The Journal of Organic ChemistryQ2 · CHEMISTRY

Synthesis of Chiral Acyclic Nucleosides by Sharpless Asymmetric Dihydroxylation: Access to Cidofovir and Buciclovir

Q2 · CHEMISTRY

Article

Author: Xie, Ming-Sheng ; Guo, Hai-Ming ; Qin, Tao ; Li, Jian-Ping ; Qu, Gui-Rong

An efficient method to construct chiral acyclic nucleosides via Sharpless asymmetric dihydroxylation of N-allylpyrimidines or N-alkenylpurines is reported. A range of chiral acyclic nucleosides with two adjacent hydroxyl groups present on the side chains could be produced in good yields (up to 97% yield) and excellent enantioselectivities (90-99% ee). The synthetic utility of the reaction was demonstrated by the catalytic asymmetric synthesis of ( S)-Cidofovir and ( R)-Buciclovir.

01 Dec 2000·Molecular PharmacologyQ3 · MEDICINE

Selective Abolishment of Pyrimidine Nucleoside Kinase Activity of Herpes Simplex Virus Type 1 Thymidine Kinase by Mutation of Alanine-167 to Tyrosine

Q3 · MEDICINE

Article

Author: Balzarini, Jan ; Degreve, Bart ; Esnouf, Robert ; De Clercq, Erik

Herpes simplex virus type 1 (HSV-1) encodes a thymidine kinase (TK) that markedly differs from mammalian nucleoside kinases in terms of substrate specificity. It recognizes both pyrimidine 2'-deoxynucleosides and a variety of purine nucleoside analogs. Based on a computer modeling study and in an attempt to modify this specificity, an HSV-1 TK mutant enzyme containing an alanine-to-tyrosine mutation at amino acid position 167 was constructed. Compared with wild-type HSV-1 TK, the purified mutant HSV-1 TK(A167Y) enzyme was heavily compromised in phosphorylating pyrimidine nucleosides such as (E)-5-(2-bromovinyl)-2'-deoxyuridine and the natural substrate dThd, whereas its ability to phosphorylate the purine nucleoside analogs ganciclovir (GCV) and lobucavir was only reduced approximately 2-fold. Moreover, a markedly decreased competition of natural pyrimidine nucleosides (i.e., thymidine) with purine nucleoside analogs for phosphorylation by HSV-1 TK(A167Y) was observed. Human osteosarcoma cells transduced with the wild-type HSV-1 TK gene were extremely sensitive to the cytostatic effects of antiherpetic pyrimidine [i.e., (E)-5-(2-bromovinyl)-2'-deoxyuridine] and purine (i.e., GCV) nucleoside analogs. Transduction with the HSV-1 TK(A167Y) gene sensitized the osteosarcoma cells to a variety of purine nucleoside analogs, whereas there was no measurable cytostatic activity of pyrimidine nucleoside analogs. The unique properties of the A167Y mutant HSV-1 TK may give this enzyme a therapeutic advantage in an in vivo setting due to the markedly reduced dThd competition with GCV for phosphorylation by the HSV-1 TK.

01 Jun 2000·Journal of Molecular Structure: THEOCHEM

Use of molecular topology in the selection of new cytostatic drugs

Author: Gomez-Lechon, M. J. ; Garcia-Domenech, R. ; Castell, J. V. ; Galvez, J.

Connectivity indexes are the topol. descriptors that are able to predict different chem. and biol. properties of the organic compoundsRecently, our research group has demonstrated their usefulness in selecting new cytostatic compounds, all of them showing antibacterial activity.In this paper we realize that this ability is considerably increased by using our home-made pharmacol. distribution diagrams (PDDs) together with the topol. charge indexes, so that the efficient selection of new candidates within heterogeneous sets of compounds is possible.This is a straightforward way for the design and/or selection of new active compounds on virtually any type of pharmacol. activity.In the present work it is demonstrated that the discovery of new cytostatic agents, potentially interesting as antineoplastics, which are in vitro active against two different cellular cultures: HepG2, human hepatocellular carcinoma and HeLa (ATCC CCL2) cell line, corresponding to the human cervix epithelioid carcinoma, is possible.Among the selected active compounds stands 6-azauridine and quinine monohydrochloride dihydrate, which show significant anti-proliferative activity on the three selected lines.Other compounds such as 1-thio-beta-d-glucose tetraacetate, di-Et 3,4-furandicarboxylate and tetrahydrofuran-2R,3T,4T,5C-tetra-carboxilic acid, show moderate inhibitory effect on CECH, and Et diethoxyacetate also exhibits moderate antiproliferative effect on HeLa and HepG2 lines.These results are important as new potential low-toxicity anticancer drugs indicate to be a possible therapy and also because mol. topol. is demonstrated to be a powerful tool for the search of new leads, completely ignoring their mechanisms of action.

100 Deals associated with Buciclovir

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Buciclovir

Overview

Basic Info

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R&D Status

Clinical Result

Translational Medicine

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Clinical Trial

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