scholarly journals Total synthesis and biological evaluation of fluorinated cryptophycins

2012 ◽  
Vol 8 ◽  
pp. 2060-2066 ◽  
Author(s):  
Christine Weiß ◽  
Tobias Bogner ◽  
Benedikt Sammet ◽  
Norbert Sewald
Keyword(s):  
Total Synthesis ◽  
Tumor Cell ◽  
Biological Evaluation ◽  
Significant Loss ◽  
Drug Resistant ◽  
Tumor Cell Lines ◽  
Cytotoxicity Assays ◽  
The Past ◽  
Highly Active ◽  
Synthesis And Biological Evaluation

Cryptophycins are cytotoxic natural products that exhibit considerable activities even against multi-drug-resistant tumor cell lines. As fluorinated pharmaceuticals have become more and more important during the past decades, fluorine-functionalized cryptophycins were synthesized and evaluated in cell-based cytotoxicity assays. The unit A trifluoromethyl-modified cryptophycin proved to be highly active against KB-3-1 cells and exhibited an IC50 value in the low picomolar range. However, the replacement of the 3-chloro-4-methoxyphenyl-substituent in unit B by a pentafluorophenyl moiety resulted in a significant loss of activity.

Synthesis and biological evaluation of novel derivatives of gambogenic acid as anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.

Design, synthesis and biological evaluation of rhein derivatives as anticancer agents

MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1812-1818 ◽  
Author(s):  
Junkai Huang ◽  
Zhuo Zhang ◽  
Peng Huang ◽  
Liqin He ◽  
Yong Ling
Keyword(s):  
Tumor Cell ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Promising Candidate ◽  
Design Synthesis ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of rhein were synthesized and evaluated for their in vitro antiproliferative activity against six kinds of tumor cell lines. All derivatives displayed more potent anti-tumor activity than rhein, and most of them were even stronger than 5-FU. Compound 4v was the most promising candidate among the investigated compounds.

Synthesis and Biological Evaluation of Novel 4,5,6,7-Tetrahydrobenzo[D]-Thiazol-2- Yl Derivatives Derived from Dimedone with Anti-Tumor, C-Met, Tyrosine Kinase and Pim-1 Inhibitions

2019 ◽  
Vol 19 (12) ◽  
pp. 1438-1453 ◽  
Author(s):  
Rafat M. Mohareb ◽  
Amr S. Abouzied ◽  
Nermeen S. Abbas
Keyword(s):  
Tyrosine Kinase ◽  
Tumor Cell ◽  
Cell Lines ◽  
Single Molecule ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
New Drugs ◽  
Tumor Cell Lines ◽  
Thiazole Derivatives ◽  
Wide Range

Background: Dimedone and thiazole moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. Thiazole derivatives are a very important class of compounds due to their wide range of pharmaceutical and therapeutic activities. On the other hand, dimedone is used to synthesize many therapeutically active compounds. Therefore, the combination of both moieties through a single molecule to produce heterocyclic compounds will produce excellent anticancer agents. Objective: The present work reports the synthesis of 47 new substances belonging to two classes of compounds: Dimedone and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. To achieve this goal, our strategy was to synthesize a series of 4,5,6,7-tetrahydrobenzo[d]-thiazol-2-yl derivatives using the reaction of the 2-bromodimedone with cyanothioacetamide. Methods: The reaction of 2-bromodimedone with cyanothioacetamide gave the 4,5,6,7-tetrahydrobenzo[d]- thiazol-2-yl derivative 4. The reactivity of compound 4 towards some chemical reagents was observed to produce different heterocyclic derivatives. Results: A cytotoxic screening was performed to evaluate the performance of the new derivatives in six tumor cell lines. Thirteen compounds were shown to be promising toward the tumor cell lines which were further evaluated toward five tyrosine kinases. Conclusion: The results of antitumor screening showed that many of the tested compounds were of high inhibition towards the tested cell lines. Compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 21b, 21c, 20d and 21d were the most potent compounds toward c-Met kinase and PC-3 cell line. The most promising compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 20c, 20d, 21b, 21c and 21d were further investigated against tyrosine kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 6c, 11b, 11d, 14b, 15c, and 20d were selected to examine their Pim-1 kinase inhibition activity the results revealed that compounds 11b, 11d and 15c had high activities.

scholarly journals Xylochemical Synthesis and Biological Evaluation of Shancigusin C and Bletistrin G

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3224
Author(s):  
Leander Geske ◽  
Ulrich Kauhl ◽  
Mohamed E. M. Saeed ◽  
Anja Schüffler ◽  
Eckhard Thines ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Aromatic Substitution ◽  
Substitution Reactions ◽  
Total Syntheses ◽  
Wittig Olefination ◽  
Starting Point ◽  
Perkin Reaction ◽  
Synthesis And Biological Evaluation

The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regioselective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.

Total synthesis and biological evaluation of Wewakazole

2017 ◽  
Vol 33 (6) ◽  
pp. 890-894 ◽  
Author(s):  
Bohua Long ◽  
Jingzhao Zhang ◽  
Xueyan Wang ◽  
Xudong Tang ◽  
Zhengzhi Wu
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Total Synthesis and Biological Evaluation of Cortistatins A and J and Analogues Thereof

2009 ◽  
Vol 131 (30) ◽  
pp. 10587-10597 ◽  
Author(s):  
K. C. Nicolaou ◽  
Xiao-Shui Peng ◽  
Ya-Ping Sun ◽  
Damien Polet ◽  
Bin Zou ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

A constitutively active ErbB4 mutant inhibits drug-resistant colony formation by the DU-145 and PC-3 human prostate tumor cell lines

2003 ◽  
Vol 192 (1) ◽  
pp. 67-74 ◽  
Author(s):  
Eric E Williams ◽  
Laurie J Trout ◽  
Richard M Gallo ◽  
Sarah E Pitfield ◽  
Ianthe Bryant ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Colony Formation ◽  
Prostate Tumor ◽  
Human Prostate ◽  
Drug Resistant ◽  
Tumor Cell Lines ◽  
Human Prostate Tumor ◽  
Prostate Tumor Cell ◽  
Constitutively Active
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