scholarly journals Synthesis, Antitumor Activity, and Docking Analysis of New Pyrido[3’,2’:4,5]furo(thieno)[3,2-d]pyrimidin-8-amines

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3952 ◽  
Author(s):  
Sirakanyan ◽  
Spinelli ◽  
Geronikaki ◽  
Hakobyan ◽  
Sahakyan ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Heterocyclic Compounds ◽  
Phosphorus Oxychloride ◽  
Docking Analysis ◽  
Structure Activity ◽  
Biological Tests ◽  
Amino Derivatives ◽  
Chloro Derivatives ◽  
Derivatives Of

Continuing our research in the field of new heterocyclic compounds, herein we report on the synthesis and antitumor activity of new amino derivatives of pyrido[3’,2’:4,5](furo)thieno[3,2-d]pyrimidines as well as of two new heterocyclic systems: furo[2–e]imidazo[1,2-c]pyrimidine and furo[2,3-e]pyrimido[1,2-c]pyrimidine. Thus, by refluxing the 8-chloro derivatives of pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidines with various amines, the relevant pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidin-8-amines were obtained. Further, the cyclization of some amines under the action of phosphorus oxychloride led to the formation of new heterorings: imidazo[1,2-c]pyrimidine and pyrimido[1,2-c]pyrimidine. The possible antitumor activity of the newly synthesized compounds was evaluated in vitro. The biological tests evidenced that some of them showed pronounced antitumor activity. A study of the structure–activity relationships revealed that the compound activity depended mostly on the nature of the amine fragments. A docking analysis was also performed for the most active compounds.

Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Human Carcinoma Cell ◽  
Ic50 Values ◽  
Relationship Of

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

ChemInform Abstract: SYNTHESIS AND ANTITUMOR ACTIVITY OF 6-OXO-7-AMINO DERIVATIVES OF 5H-PYRIDO(2,3B)- AND 5H-PYRIMIDO(4,5B)(1,4)THIAZINES

1985 ◽  
Vol 16 (15) ◽  
Author(s):  
N. I. TRAVEN' ◽  
YU. A. ERSHOVA ◽  
A. S. SOKOLOVA ◽  
V. A. CHERNOV ◽  
T. S. SAFONOVA
Keyword(s):  
Antitumor Activity ◽  
Amino Derivatives ◽  
Derivatives Of

Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Schiff Base Derivatives ◽  
In Vivo Antitumor Activity ◽  
Derivatives Of

scholarly journals Structure-activity studies of 20-deoxo-20-amino derivatives of tylosin-related macrolides.

1989 ◽  
Vol 42 (11) ◽  
pp. 1673-1683 ◽  
Author(s):  
H. A. KIRST ◽  
K. E. WILLARD ◽  
M. DEBONO ◽  
J. E. TOTH ◽  
B. A. TRUEDELL ◽  
...  
Keyword(s):  
Structure Activity ◽  
Amino Derivatives ◽  
Derivatives Of

2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity

1993 ◽  
Vol 36 (23) ◽  
pp. 3611-3617 ◽  
Author(s):  
Maria Bretner ◽  
Tadeusz Kulikowski ◽  
Jolanta M. Dzik ◽  
Malgorzata Balinska ◽  
Wojciech Rode ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Thymidylate Synthase ◽  
Derivatives Of

New anthrahydrazone derivatives and their cisplatin-like complexes: synthesis, antitumor activity and structure–activity relationship

2019 ◽  
Vol 43 (47) ◽  
pp. 18685-18694 ◽  
Author(s):  
Rui-Xue Liu ◽  
Ying-Shu Wu ◽  
Yan-Cheng Liu ◽  
Ru-Yi Luo ◽  
Li-Dong Yang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Two new cisplatin-like platinum(ii) complexes of new anthrahydrazones showed significant in vitro antitumor efficacies, which were totally different from that of cisplatin.

Synthesis and In Vitro Antitumor Activity of Novel Ring D Analogues of the Marine Pyridoacridine Ascididemin: Structure−Activity Relationship

2002 ◽  
Vol 45 (17) ◽  
pp. 3765-3771 ◽  
Author(s):  
Evelyne Delfourne ◽  
Francis Darro ◽  
Philippe Portefaix ◽  
Chantal Galaup ◽  
Sylvie Bayssade ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Struktur-Wirkungsbeziehungen polyfunktioneller Diterpene des Tigliantyps, IV [1-3]. Derivate des Tiglians mit fehlendem oder geöffnetem Cyclopropanring und ihre irritierende und tumorpromovierende Wirkung / Structure-Activity Relationships of Polyfunctional Diterpenes of the Tigliane Type, IV [1-3]. Derivatives of Tigliane without or with Opened Cyclopropane Ring and their Irritant and Promoting Activity

1980 ◽  
Vol 35 (11) ◽  
pp. 1470-1475 ◽  
Author(s):  
Bernd Sorg ◽  
Michael Gschwendt ◽  
Heinz Walter Thielmann ◽  
Erich Hecker
Keyword(s):  
Cyclopropane Ring ◽  
Complete Removal ◽  
Total Loss ◽  
Structure Activity Relationships ◽  
Type Iv ◽  
Structure Activity ◽  
Biological Tests ◽  
Derivatives Of

Abstract The synthesis of the esters 6d-8d, 9 c and 10 c is described. These compounds are closely structurally related to the irritant and tumorpromoting 12-O-tetradecanoylphorbol-13-acetate (TPA, 2 a) and to phorbol-12,13-didecanoate (PDD, 2 c) except that they possess no cyclopropane ring. Biological tests show that opening or complete removal of the cyclopropane ring leads to nearly total loss of irritant or tumorpromoting (tested in the case of 9 c and 10 c) activity.

Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiose micarbazone

1992 ◽  
Vol 35 (20) ◽  
pp. 3672-3677 ◽  
Author(s):  
Mao Chin Liu ◽  
Tai Chun Lin ◽  
Alan C. Sartorelli
Keyword(s):  
Antitumor Activity ◽  
Amino Derivatives ◽  
Derivatives Of
Sign in / Sign up

Export Citation Format

Share Document