Synthesis and biological evaluation of peptidomimetics containing the tryptamine moiety as a potential antitumor agent

RSC Advances ◽  
2015 ◽  
Vol 5 (20) ◽  
pp. 15597-15602 ◽  
Author(s):  
Xiaohui Wang ◽  
Haihuan Su ◽  
Changshui Chen ◽  
Xiufang Cao
Keyword(s):  
Cell Proliferation ◽  
Cell Lines ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A series of novel peptidomimetics bearing tryptamine moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation (HepG2, Huh-7, A875 and BEL-7402/5-FU cell lines).

scholarly journals Synthesis and Biological Evaluation of Novel 4-(4-Formamidophenylamino)-N-methylpicolinamide Derivatives as Potential Antitumor Agents

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1150
Author(s):  
Nana Meng ◽  
Shuyan Zhou ◽  
Min Hu ◽  
Youzhi Xu ◽  
Yong Xia ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
Apoptosis And Necrosis ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.

Synthesis and Biological Evaluation of Diaryl Ether Linked DC-81 Conjugates as Potential Antitumor Agents

2013 ◽  
Vol 13 (10) ◽  
pp. 1590-1600 ◽  
Author(s):  
Ahmed Kamal ◽  
A. Viswanath ◽  
M. Ramaiah ◽  
J. Murty ◽  
Farheen Sultana ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Diaryl Ether ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents

2011 ◽  
Vol 46 (12) ◽  
pp. 5970-5977 ◽  
Author(s):  
Hongbin Zou ◽  
Liang Zhang ◽  
Jingfeng Ouyang ◽  
Marc A. Giulianotti ◽  
Yongping Yu
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

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