Design, Synthesis, and in vitro Anti-mycobacterial Activities of Propylene-tethered Heteronuclear Bis-isatin Derivatives

2018 ◽  
Vol 55 (6) ◽  
pp. 1504-1508 ◽  
Author(s):  
Xue Hua ◽  
Guifu Zhang ◽  
Deqing Zhang ◽  
Yequn Wu
Keyword(s):  
Design Synthesis ◽  
Isatin Derivatives

Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives

Fitoterapia ◽  
2018 ◽  
Vol 127 ◽  
pp. 383-386 ◽  
Author(s):  
Yan Xu ◽  
Jianguo Guan ◽  
Zhi Xu ◽  
Shijia Zhao
Keyword(s):  
Design Synthesis ◽  
Isatin Derivatives

Design, synthesis and in vitro cytotoxicity evaluation of 5-(2-carboxyethenyl)isatin derivatives as anticancer agents

2014 ◽  
Vol 24 (2) ◽  
pp. 591-594 ◽  
Author(s):  
Kailin Han ◽  
Yao Zhou ◽  
Fengxi Liu ◽  
Qiannan Guo ◽  
Pengfei Wang ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
In Vitro Cytotoxicity ◽  
Design Synthesis ◽  
Isatin Derivatives

scholarly journals Design, Synthesis, Antimicrobial and Anticancer Activity of some Novel Benzoxazole-Isatin Conjugates

2021 ◽  
Vol 12 (2) ◽  
pp. 2392-2403
Keyword(s):  
Antibacterial Activity ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Protein Targets ◽  
Human Cancer Cell Lines ◽  
Fungal Organisms ◽  
Isatin Derivatives

A series of novel benzoxazole-isatin conjugates were synthesized by treating 2-amino benzoxazole with 5 and 7 substituted isatin derivatives and were screened for in vitro antimicrobial and cytotoxic activities. The results showed that all the synthesized compounds shown mild to potent antibacterial activity. The MIC values were found between 10 and 100 µg/ml against tested bacterial and fungal organisms. Among all the compounds, 3d & 3c showed good antimicrobial. In vitro cytotoxic activities were evaluated by MTT assay of all the test compounds against the different human cancer cell lines. The compounds having substitution with electron-withdrawing groups (halides) at the 5th position on the isatin ring showed the most significant biological activity than substituted at the 7th position. The molecular docking interactions have shown good binding interactions with the protein targets glucosamine-6-phosphate synthase (GlcN-6-P synthase) and telomerase.

Tetraethylene Glycol Tethered Heteronuclear Bis-isatin Derivatives: Design, Synthesis, and In Vitro Anti-mycobacterial Activities

2018 ◽  
Vol 55 (9) ◽  
pp. 2172-2177 ◽  
Author(s):  
Shuang-Qi Zhao ◽  
Yan Xu ◽  
Jianguo Guan ◽  
Shijia Zhao ◽  
Guang-De Zhang ◽  
...  
Keyword(s):  
Tetraethylene Glycol ◽  
Design Synthesis ◽  
Isatin Derivatives

Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives

2005 ◽  
Vol 13 (9) ◽  
pp. 3249-3261 ◽  
Author(s):  
Idan Chiyanzu ◽  
Cailean Clarkson ◽  
Peter J. Smith ◽  
Julie Lehman ◽  
Jiri Gut ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Isatin Derivatives

Design, Synthesis, Molecular Docking and Biological Evaluation of 1-(benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol Derivatives as Antiproliferative Agents

2019 ◽  
Vol 16 (10) ◽  
pp. 837-845
Author(s):  
Sandhya Jonnala ◽  
Bhaskar Nameta ◽  
Murthy Chavali ◽  
Rajashaker Bantu ◽  
Pallavi Choudante ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Mouse Skin ◽  
Coupling Reaction ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin melanoma) and CHO-K1 (Chinese hamster ovary cells), a noncancerous cell line. In vitro inhibitory activity indicates that compounds 4a, 4b, 4c, 4d, 4g, 4j, and 4o exhibited potent anti-proliferative behavior. Among them, compounds 4g, 4j and 4o found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking facilitates to investigate the probable binding mode and key active site interactions in tubulins α and β proteins. The docking results are complementary to experimental results.

Discovery of N-Phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine Derivatives as Potent Mnk2 Inhibitors: Design, Synthesis, SAR Analysis, and Evaluation of in vitro Anti-leukaemic Activity

2019 ◽  
Vol 15 (6) ◽  
pp. 602-623 ◽  
Author(s):  
Ahmed M. Abdelaziz ◽  
Sarah Diab ◽  
Saiful Islam ◽  
Sunita K.C. Basnet ◽  
Benjamin Noll ◽  
...  
Keyword(s):  
Proliferative Activity ◽  
Myeloid Cell ◽  
Structural Diversity ◽  
Translation Initiation Factor ◽  
Initiation Factor ◽  
Cell Leukaemia ◽  
Aberrant Expression ◽  
Design Synthesis ◽  
Induced Apoptosis

Background:Aberrant expression of eukaryotic translation initiation factor 4E (eIF4E) is common in many types of cancer including acute myeloid leukaemia (AML). Phosphorylation of eIF4E by MAPK-interacting kinases (Mnks) is essential for the eIF4E-mediated oncogenic activity. As such, the pharmacological inhibition of Mnks can be an effective strategy for the treatment of cancer.Methods:A series of N-phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine derivatives was designed and synthesised. The Mnk inhibitory activity of these derivatives as well as their anti-proliferative activity against MV4-11 AML cells was determined.Results:These compounds were identified as potent Mnk2 inhibitors. Most of them demonstrated potent anti-proliferative activity against MV4-11 AML cells. The cellular mechanistic studies of the representative inhibitors revealed that they reduced the level of phosphorylated eIF4E and induced apoptosis by down-regulating the anti-apoptotic protein myeloid cell leukaemia 1 (Mcl-1) and by cleaving poly(ADP-ribose)polymerase (PARP). The lead compound 7k possessed desirable pharmacokinetic properties and oral bioavailability.Conclusion:This work proposes that exploration of the structural diversity in the context of Nphenyl- 4-(1H-pyrrol-3-yl)pyrimidin-2-amine would offer potent and selective Mnk inhibitors.

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