Antitumor agents. 25. Synthesis and antitumor activity of uracil and thymine .alpha.-methylene-.gamma.-lactones and related derivatives

1977 ◽  
Vol 20 (7) ◽  
pp. 911-914 ◽  
Author(s):  
Kuo-Hsiung Lee ◽  
Yih-Shiong Wu ◽  
Iris H. Hall
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals Design, Synthesis, and Antitumor Activity of Olmutinib Derivatives Containing Acrylamide Moiety

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3041
Author(s):  
Xiaohan Hu ◽  
Sheng Tang ◽  
Feiyi Yang ◽  
Pengwu Zheng ◽  
Shan Xu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Design Synthesis ◽  
Structure Activity ◽  
Excellent Activity ◽  
Ic50 Values ◽  
Mcf 7

Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, H10, showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase. The structure–activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Additionally, the substitution of different acrylamide side chains had different effects on the activity of compounds. Generally, compounds H7 and H10 were confirmed as promising antitumor agents.

Synthesis of diaminodideoxyalditol analogs of cisplatin as antitumor agents

1993 ◽  
Vol 71 (6) ◽  
pp. 880-885 ◽  
Author(s):  
S. Hanessian ◽  
J.-Y. Gauthier ◽  
K. Okamoto ◽  
A.L. Beauchamp ◽  
T. Theophanides
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Platinum Complexes ◽  
Hydroxy Groups

Acyclic vicinal polyol complexes related to cisplatin were synthesized from D-mannitol by stereocontrolled manipulation of the hydroxy groups. Controlled cleavage of a 3,4-diazido hexitol gave the corresponding D-threitol and D-xylitol analogs, which were converted to their diamino platinum complexes. The antitumor activity of these compounds is reported.

scholarly journals Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response

RSC Advances ◽  
2018 ◽  
Vol 8 (43) ◽  
pp. 24376-24385 ◽  
Author(s):  
Wen-Bin Kuang ◽  
Ri-Zhen Huang ◽  
Yi-Lin Fang ◽  
Gui-Bin Liang ◽  
Chen-Hui Yang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Quinoline Derivatives ◽  
Apoptotic Response ◽  
Design Synthesis ◽  
Cycle Arrest ◽  
In Vivo Antitumor Activity ◽  
Combination Principle

A series of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives were designed and synthesized as antitumor agents under the combination principle. The antitumor activity and mechanisms were then evaluated.

scholarly journals Screening of Antibacterial, Thrombolytic, Membrane Stabilizing, Anti-inflammatory and Antitumor Activity of Citrus assamensis Leaf Extracts

2018 ◽  
Vol 10 (2) ◽  
pp. 195-210
Author(s):  
M. Shahriar ◽  
M. A. Bhuiyan ◽  
M. S. Rana
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Chloroform Extract ◽  
Haemolytic Activity ◽  
Hypotonic Solution ◽  
Leaf Extracts ◽  
Thrombolytic Activity ◽  
Anti Inflammatory

The methanol, ethanol and chlorofom leaf extracts of Satkara, Citrus assamensis (family: Rutaceae), were subjected to in vitro anti-bacterial, thrombolytic, membrane stabilizing and in vivo anti-inflammatory and antitumor activity tests. The chloroform extract of C. assamensis showed the most important spectrum of activity against Bacillus subtilis, Bacillus cereus, Sarcina lutea among 6 gram positive and against 11 gram negative bacteria at the concentration of 1000 μg/disc, while the range of zones of inhibition were within 7-16 mm. Among the tested three extracts CHCl3 extract showed potent thrombolytic activity and hypotonic solution induced haemolytic activity where the percentages of inhibition were found to be 35% and 55% respectively. All the extracts established significant (p<0.05) anti-inflammatory effect by regulating biphasic inflammatory process induced by carrageenan. The leaf extract dose-dependently and significantly decreases the number of EAC cell count and inhibition of cell growth in comparison to the EAC control and standard. The results obtained in the present study indicate that, C. assamensis leaf can be a potential source of anti-bacterial, thrombolytic, membrane stabilizing, anti-inflammatory and antitumor agents.

Hydrophilic analogs of (R,R)-diaminocyclohexane dichloroplatinum (DACH) and the influence of relative stereochemistry on antitumor activity

1993 ◽  
Vol 71 (12) ◽  
pp. 2102-2108 ◽  
Author(s):  
Stephen Hanessian ◽  
Jianguo Wang
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Platinum Complex ◽  
Cyclohexane Ring ◽  
P388 Leukemia ◽  
Relative Stereochemistry ◽  
Leaving Groups ◽  
Hydroxy Groups

A series of analogs of (R,R)-1,2-diaminocyclohexane dichloroplatinum(II) (DACH) containing stereochemically defined hydroxy groups and appropriate acidic leaving groups were synthesized and tested as antitumor agents. The (1α,2β,3α,4β)-1,4-dihydroxy-2,3-diaminocyclohexane analog showed the highest potency against P388 leukemia in mice. The results indicate that increasing the hydrophilicity of the platinum complex to a certain extent could improve the antitumor activity of the drug. It is also likely that the stereochemical disposition of the substituents on the cyclohexane ring affects the antitumor activity.

Potential antitumor agents. 54. Chromophore requirements for in vivo antitumor activity among the general class of linear tricyclic carboxamides

1988 ◽  
Vol 31 (4) ◽  
pp. 707-712 ◽  
Author(s):  
Brian D. Palmer ◽  
Gordon W. Rewcastle ◽  
Graham J. Atwell ◽  
Bruce C. Baguley ◽  
William A. Denny
Keyword(s):  
Antitumor Activity ◽  
General Class ◽  
Antitumor Agents ◽  
In Vivo Antitumor Activity ◽  
Potential Antitumor
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