Diarylsemicarbazones: synthesis, antineoplastic activity and topoisomerase I inhibition assay
摘要:
A series of diarylsemicarbazones was synthesized and tested against human neoplastic cell lines. The more active members have a 1-naphthyl ring at the carbamidic nitrogen, and chloro, dimethylamino or nitro group substituents at the benzylidene moiety. None of these showed affinity to DNA. One of the more active compounds was tested as a topoisomerase I inhibitor and showed a potent effect. SAR studies demonstrated linear correlation between lypophilicity and activity on the most sensitive lines and a definite conformational shape for antineoplastic action. (C) 1999 Elsevier Science S.A. All rights reserved.
Substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs as activators of caspases and inducers of apoptosis and the use thereof
申请人:——
公开号:US20020128292A1
公开(公告)日:2002-09-12
The present invention is directed to substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs thereof, represented by the general Formula I:
1
wherein X, Ar
1
, R
2
-R
6
and R
12
are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides, processes for their preparation and pharmaceutical uses thereof
申请人:FERRER INTERNACIONAL, S.A.
公开号:EP1803722A1
公开(公告)日:2007-07-04
The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R1, R2 and R3 have different meanings, and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediate compounds thereof.
Oxygenation of aromatic ketone hydrazones with Co(salen) in methanol resulted unexpectedly in oxidative degradation to give methyl benzoate derivatives. A mechanism involving nucleophilic attack by methanol on a diazo intermediate is discussed.
[EN] N-ACYLHYDRAZONE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS<br/>[FR] DÉRIVÉS DE N-ACYLHYDRAZONE UTILES COMME MODULATEURS DES RÉCEPTEURS NICOTINIQUES DE L'ACÉTYLCHOLINE
申请人:NEUROSEARCH AS
公开号:WO2009065854A1
公开(公告)日:2009-05-28
This invention relates to N-acylhydrazone derivatives (I), which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.