In-Vitro Anti-HIV and Antitumor Activity of New 3,6-Disubstituted [1,2,4]Triazolo[3,4-b][1,3,4]thiadiazoles and Thiadiazine Analogues

A series of [1,2,4]triazolo[3,4‐b][1,3,4]thiadiazoles (7–15) and the thiadiazine analogues 16–18 have been synthesized under microwave irradiation (MWI). All synthesized compounds are evaluated for their antiviral activity against the replication of HIV‐1 and HIV‐2 activity in MT‐4. However, compoun...

Full description

Saved in:
Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2008-06, Vol.341 (6), p.365-369
Main Authors: Al-Soud, Yaseen A., Al-Masoudi, Najim A., Loddo, Robert, La Colla, Paola
Format: Article
Language:English
Subjects:
Anti-HIV activity
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - pharmacology
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Antitumor activity
Cell Line
Cell Line, Tumor
Drug Screening Assays, Antitumor
HIV-1 - drug effects
HIV-2 - drug effects
Human immunodeficiency virus
Human immunodeficiency virus 1
Human immunodeficiency virus 2
Humans
Microwave-assisted synthesis
Structure-Activity Relationship
T-Lymphocytes - drug effects
T-Lymphocytes - virology
Thiadiazines
Thiadiazines - chemical synthesis
Thiadiazines - pharmacology
Thiadiazoles - chemical synthesis
Thiadiazoles - pharmacology
Triazoles - chemical synthesis
Triazoles - pharmacology
Triazolothiadiazoles
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of [1,2,4]triazolo[3,4‐b][1,3,4]thiadiazoles (7–15) and the thiadiazine analogues 16–18 have been synthesized under microwave irradiation (MWI). All synthesized compounds are evaluated for their antiviral activity against the replication of HIV‐1 and HIV‐2 activity in MT‐4. However, compounds 12 and 18 showed EC50 = 2.11 and 1.97 μg/mL. The results suggest that these compounds can be considered as a new lead in the development of antiviral agents. Compounds 4–18 were tested in vitro against a panel of tumor cell lines. All compounds are inactive against all the tumor sub‐lines, except 10 which exhibited activity against CD4+ human acute T‐lymphoblastic leukaemia of CC50 = 64 μM.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.200700272