80258-99-7Relevant academic research and scientific papers
A nitrogen hetero-cycloalkyl amino quinacridineone-4-amide compound and its preparation method and application
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, (2017/01/31)
The invention provides an azo-heteroaromatic cycloalkylaminoacridone-4-amide compound which is shown in a formula I or a formula II as shown in the specification, as well as a preparation method and application thereof. In the formula I and the formula II
Molecular design, synthesis and biological research of novel pyridyl acridones as potent DNA-binding and apoptosis-inducing agents
Zhang, Bin,Chen, Kang,Wang, Ning,Gao, Chunmei,Sun, Qinsheng,Li, Lulu,Chen, Yuzong,Tan, Chunyan,Liu, Hongxia,Jiang, Yuyang
, p. 214 - 226 (2015/03/04)
A series of novel pyridyl acridone derivatives comprised of a pseudo-five-cyclic system to extend the π-conjugated acridone chromophore, were designed and synthesized as potent DNA binding antitumor compounds. Most synthesized compounds displayed good act
Potential Antitumor Agents. 46. Structure-Activity Relationships for Acridine Monosubstituted Derivatives of the Antitumor Agent N--9-aminoacridine-4-carboxamide
Rewcastle, Gordon W.,Atwell, Graham J.,Chambers, David,Baguley, Bruce C.,Denny, William A.
, p. 472 - 477 (2007/10/02)
A series of monosubstituted derivatives of the new antitumor agent N--9-aminoacridine-4-carboxamide has been prepared, bearing methyl, methoxy, and chloro groups at available acridine positions.The physicochemical properties and an
Synthesis of Substituted 9-Oxo-9,10-dihydroacridine-4-carboxylic Acids. I. Factors Affecting the Direction of Ring Closure of Substituted N-(2-Carboxyphenylamino)benzoic Acids
Stewart, Georgina M.,Rewcastle, Gordon W.,Denny, William A.
, p. 1939 - 1950 (2007/10/02)
The cyclodehydration of 16 substituted N-(2-carboxyphenylamino)benzoic acids to substituted 9-oxo-9,10-dihydroacridine-4-carboxylic acids with conc.H2SO4, POCl3 and ethyl polyphosphate (epp) has been studied by h.p.l.c.Direction of ring closure can be qua
Potential antitumor agents. 38. 3-Substituted 5-carboxamido derivatives of amsacrine
Denny,Atwell,Baguley
, p. 1619 - 1625 (2007/10/02)
The synthesis and biological evaluation of a series of 3-substituted 5-carboxamido derivatives of amsacrine (m-AMSA) are described. This series was developed as the result of previous quantitative structure-activity relationship (QSAR) studies of the antitumor activity of 9-anilinoacridine derivatives. In agreement with these studies, this class of compounds, possessing a variety of small nonpolar groups at the 3-position, together with very hydrophilic carboxamido groups at the 5-position, have high in vivo activity against animal leukemia models.
Potential Antitumor Agents. 36. Quanitative Relationships between Experimental Antitumor Activity, Toxicity, and Structure for the General Class of 9-Anilinoacridine Antitumor Agents
Denny, William A.,Cain, Bruce F.,Atwell, Graham J.,Hansch, Corwin,Panthananickal, Augustine,Leo, A.
, p. 276 - 300 (2007/10/02)
Quantitative relationships (QSAR) have been derived between antileukemic (L1210) activity and agent physicochemical properties for 509 tumor-active members of the general class of 9-anilinoacridines.One member of this class is the clinical agent m-AMSA (NSC 249992).Agent hydrophobicity proved a significant but not a dominant influence on in vivo potency.The electronic properties of substituent groups proved important, but the most significant effects on drug potency were shown by the steric influence of groups placed at various positions on the 9-anilinoacridine skeleton.The results are entirely consistent with the physiologically important step in the action of these compounds being their binding to double-stranded DNA by intercalation of the acridine chromophore between the base pairs and positioning of the anilino group in the minor groove, as previously suggested.An equation was also derived for the acute toxicities of 643 derivatives of 9-anilinoacridine.This equation took a somewhat similar form to the one modeling antileukemia potency, emphasizing the usual fairly close relationship between potency and acute toxicity for antitumor agents in general.This study demonstrated the power of QSAR techniques to structure very large amounts of biological data and to allow the extraction of useful information from bearing on the possible site of action of the compounds concerned.
